Product Overview

Tranexamic Acid (TXA, INCI: Tranexamic Acid, trans-4-(Aminomethyl)cyclohexanecarboxylic acid, CAS 1197-18-8, C₈H₁₅NO₂, MW 157.21 g/mol, EINECS 214-818-2) is a synthetic lysine analog originally developed as an antifibrinolytic hemostatic pharmaceutical that has emerged as one of the most effective skin brightening actives in cosmetic dermatology. TXA operates through a unique dual mechanism that no other brightening active replicates: (1) Plasminogen/plasmin pathway inhibition — UV radiation converts plasminogen to plasmin in epidermal keratinocytes; plasmin triggers arachidonic acid release and prostaglandin E2 (PGE2) production, which directly stimulates melanogenesis in melanocytes. TXA blocks plasminogen activation at the lysine-binding site, interrupting the UV → plasmin → arachidonic acid → PGE2 → melanin signaling cascade upstream of tyrosinase. (2) Competitive tyrosinase inhibition — TXA structurally resembles L-tyrosine and occupies the tyrosinase active site, blocking melanin synthesis at the rate-limiting enzymatic step. This dual mechanism — upstream plasmin signal blockade + downstream tyrosinase inhibition — provides 50× the brightening efficacy of vitamin C on a molar basis and approximately 10× the potency of AHA for reducing dark spots. First reported for melasma treatment in 1979, TXA is now supported by a 2024 meta-analysis of 28 RCTs confirming significant melasma and PIH reduction. UPOR Biotech provides tranexamic acid in two grades: Pharma grade (≥99% HPLC, USP/EP/BP/JP monograph compliant) with Type II DMF support, and Cosmetic grade (≥98% HPLC) optimized for topical formulations.

As a leading tranexamic acid manufacturer and bulk supplier, UPOR Biotech provides high-purity TXA powder for B2B cosmetic brands, pharmaceutical companies, contract manufacturers, and private-label formulators worldwide. TXA’s dual pharma + cosmetic positioning creates unique market opportunities — particularly for premium cosmeceutical lines, dermatologist-dispensed products, and companies operating across both pharmaceutical and cosmetic markets. OEM and private label formulations available with flexible MOQ starting at 1 kg. Free sample available for qualified buyers. Every shipment includes full documentation: COA, MSDS, HPLC chromatogram, and stability data.

Tranexamic Acid vs Kojic Acid vs Alpha Arbutin — Three-Pathway Brightening: Why TXA Is the Plasmin Signal Blocker the Others Can’t Replace

Comparing the three leading non-hydroquinone brightening actives reveals complementary — not competitive — mechanisms. Kojic Acid works downstream by chelating copper at the tyrosinase active site; it provides the fastest initial brightening but carries a 12–63% contact sensitization risk and is prone to oxidative yellowing in formulations. Alpha Arbutin is a slow-release competitive tyrosinase inhibitor — the gentlest and most stable option, ideal for sensitive skin and daily maintenance, but slower to show visible results (6–12 weeks). Tranexamic Acid is unique: it blocks the upstream plasmin activation signal — the molecular “overproduction command” that triggers melanogenesis before tyrosinase even activates. This is the pathway that neither kojic acid nor α-arbutin addresses. TXA is 50× more potent than vitamin C on a molar basis, has the strongest clinical evidence for melasma (28 RCTs, 2024 meta-analysis), and carries negligible irritation risk. The optimal formulation strategy: TXA (plasmin blockade) + α-Arbutin (tyrosinase inhibition) + Niacinamide (melanosome transfer inhibition) = complete three-control-point brightening with zero cytotoxicity, global regulatory compliance, and suitability for all Fitzpatrick skin types.

Technical Specifications

PropertySpecification
Product NameTranexamic Acid Powder — Pharma Grade (≥99% USP/EP) / Cosmetic Grade (≥98%)
INCI NameTranexamic Acid
Common Name / SynonymsTXA; trans-4-(Aminomethyl)cyclohexanecarboxylic acid; trans-AMCHA; Cyclohexamic acid; trans-4-(Aminomethyl)cyclohexane carboxylic acid
CAS Number1197-18-8
Molecular FormulaC₈H₁₅NO₂
Molecular Weight157.21 g/mol
SourceSynthetic — synthetic lysine analog
Key AdvantageDual mechanism: plasminogen/plasmin pathway inhibition (upstream signal blockade) + competitive tyrosinase inhibition. 50× vitamin C molar potency. Only brightening active targeting the plasmin pathway.
AppearanceWhite or almost white crystalline powder
Assay (Pharma Grade)≥99.0% (HPLC, anhydrous basis) — USP/EP/BP/JP monograph compliant
Assay (Cosmetic Grade)≥98.0% (HPLC, anhydrous basis)
IdentificationIR spectrum conforms to reference standard; HPLC retention time matches USP/EP Tranexamic Acid RS
Loss on Drying≤0.5% (105°C, 2 hours)
Residue on Ignition≤0.1%
pH (1% Aqueous Solution)6.5 – 7.5
SolubilityFreely soluble in water (≥100 mg/mL at 25°C); practically insoluble in ethanol (96%) and acetone
Chloride (Cl)≤0.014% (USP/EP limit)
Heavy Metals (Total)≤10 ppm (as Pb)
Elemental ImpuritiesPb ≤2 ppm; As ≤1 ppm; Hg ≤1 ppm; Cd ≤1 ppm (USP <232> / ICH Q3D compliant)
Microbial LimitsTAMC ≤100 CFU/g; TYMC ≤10 CFU/g (USP <61> / EP <2.6.12>); Pathogens (E. coli, Salmonella, S. aureus, P. aeruginosa) — Absent in 10 g (USP <62> / EP <2.6.13>)
Residual SolventsUSP <467> / EP <5.4> / ICH Q3C Class 3 compliant
Recommended Usage (Cosmetic)0.5 – 3.0%; 2.0% most common for brightening efficacy. Add directly to aqueous phase at room temperature.
Grade / StandardsPharma Grade (≥99%, USP/EP/BP/JP monograph compliant) / Cosmetic Grade (≥98% HPLC)
DMFType II Drug Master File support available (pharma grade)
CertificationsISO 9001:2015, ISO 22000, HACCP, FDA Facility Registration, HALAL, KOSHER, Non-GMO, BSE/TSE-Free
Packaging1 kg / 5 kg / 10 kg sealed aluminum foil bags with PE liner; 25 kg fiber drums with double PE liner
Storage15 – 25°C, tightly sealed in original container, protect from light and moisture
Shelf Life3 years from date of manufacture under recommended storage conditions

Key Benefits — Tranexamic Acid

Dual-Mechanism Brightening — Plasmin Signal Blockade + Tyrosinase Inhibition

TXA’s unique dual pathway: blocks UV-induced plasmin activation at the keratinocyte lysine-binding site — the upstream “overproduction command” that triggers melanogenesis — AND competitively inhibits tyrosinase at the rate-limiting enzymatic step. No other brightening active targets the plasmin pathway.

Dual Pathway

50× Vitamin C Molar Potency — Clinically Proven for Melasma & PIH

On a molar basis, TXA provides 50× the brightening potency of vitamin C and 10× the potency of AHA. Supported by a 2024 meta-analysis of 28 RCTs confirming significant melasma and post-inflammatory hyperpigmentation reduction. The most clinically validated non-hydroquinone brightening active available.

50× Vitamin C

Pharma + Cosmetic Dual-Grade — USP/EP Monograph with DMF Support

Pharma grade (≥99% HPLC, USP/EP/BP/JP) with Type II DMF support for Rx and premium cosmeceutical products. Cosmetic grade (≥98% HPLC) optimized for topical formulations. Both grades available with full documentation — COA, MSDS, HPLC chromatogram, and stability data.

USP/EP + DMF

Non-Cytotoxic, Non-Irritating — Safe for All Fitzpatrick Skin Types

Unlike hydroquinone, TXA does not kill melanocytes. Non-irritating, non-sensitizing, and clinically safe for long-term daily use across all Fitzpatrick skin types I–VI — including darker tones most prone to PIH. pH stable 4–8. Compatible with all standard cosmetic ingredients.

All Skin Types

Applications

Melasma & Hyperpigmentation Treatment Serums

TXA at 2–3% in targeted melasma and hyperpigmentation serums. The most effective non-hydroquinone active for stubborn pigmentation. OEM and private label formulations available with flexible MOQ starting at 1 kg.

Premium Cosmeceutical Brightening Ampoules

Pharma-grade TXA (≥99% USP/EP) at 2% in premium cosmeceutical ampoules and professional skincare lines. DMF support available for dermatologist-dispensed and Rx-cosmetic hybrid product positioning.

Post-Procedure PIH Prevention & Aftercare

TXA prevents and treats post-inflammatory hyperpigmentation after laser, chemical peel, and microneedling procedures. The plasmin inhibition mechanism directly targets the UV- and trauma-induced pigmentation signaling pathway.

Daily Brightening Moisturizers & UV Protection

TXA at 0.5–1% in daily moisturizers, sunscreens, and BB/CC creams for maintenance brightening. Combined with broad-spectrum UV filters for comprehensive photo-pigmentation protection — prevent + correct in a single product.

Oral Tranexamic Acid — Hemostatic Pharmaceuticals

Pharma-grade TXA (≥99% USP/EP/BP/JP) for oral and injectable hemostatic pharmaceutical formulations. Type II DMF support available. Dual pharma + cosmetic positioning for companies operating across both regulated markets.

Brightening Body Care & Inclusive Even-Tone Formulations

TXA at 1–2% in body lotions, underarm, intimate area, and full-body brightening products. Growing global market for inclusive body care and even-tone formulations. Non-irritating and safe for sensitive skin areas.

Frequently Asked Questions

Tranexamic Acid (TXA, CAS 1197-18-8) is a synthetic lysine analog with a dual brightening mechanism that no other active replicates. (1) Plasminogen/plasmin pathway inhibition — UV radiation converts plasminogen to plasmin in epidermal keratinocytes; plasmin triggers arachidonic acid → PGE2 → melanogenesis. TXA blocks this cascade at the plasmin activation step — upstream of tyrosinase — by occupying keratinocyte lysine-binding sites. (2) Competitive tyrosinase inhibition — TXA structurally resembles L-tyrosine and occupies the tyrosinase active site. This dual mechanism provides 50× vitamin C molar potency and approximately 10× AHA potency for dark spot reduction. First reported for melasma in 1979, TXA is now supported by a 2024 meta-analysis of 28 RCTs confirming significant efficacy. TXA is particularly effective for UV-induced hyperpigmentation, melasma, and PIH — conditions driven by the plasmin signaling pathway. UPOR Biotech provides both pharma (≥99% USP/EP, with DMF) and cosmetic (≥98%) grades.

TXA delivers four key benefits for cosmetic formulators and brands: (1) 50× vitamin C brightening potency on a molar basis via dual plasmin + tyrosinase inhibition — the most potent non-hydroquinone brightening mechanism available. (2) Clinically proven melasma and PIH reduction — a 2024 meta-analysis of 28 RCTs confirmed significant mMASI score reduction (p = 0.02) and quality-of-life improvement (p = 0.03). (3) Non-cytotoxic safety — unlike hydroquinone, TXA does not kill melanocytes and is safe for all Fitzpatrick skin types I–VI, including darker tones most prone to PIH. (4) Excellent formulation flexibility — freely water-soluble (≥100 mg/mL at 25°C), pH stable from 4–8, compatible with niacinamide, vitamin C, α-arbutin, and virtually all standard cosmetic ingredients. Primary applications: melasma serums (2–3%), cosmeceutical ampoules (2%), post-procedure PIH aftercare, daily brightening moisturizers (0.5–1%), oral hemostatic pharmaceuticals (pharma grade), and inclusive body care formulations.

Cosmetic usage rate: 0.5–3.0% in leave-on formulations. 2.0% is the most common and clinically validated concentration for brightening efficacy. TXA is freely water-soluble (≥100 mg/mL at 25°C) — add directly to the aqueous phase at room temperature; no heating, pre-dissolution, or co-solvents required. pH stable from 4–8; no special buffering needed. Compatible with virtually all standard cosmetic ingredients including niacinamide, vitamin C (L-ascorbic acid), α-arbutin, kojic acid, AHAs, BHAs, peptides, and preservatives. The gold-standard brightening combination: TXA 2% + Niacinamide 4–5% + α-Arbutin 1% — providing comprehensive coverage across all three melanogenesis control points: plasmin activation signal blockade (TXA), tyrosinase inhibition (α-arbutin), and melanosome transfer inhibition (niacinamide). For topical + microneedling protocols, TXA shows enhanced epidermal penetration and superior melasma outcomes per the 2024 meta-analysis. Always formulate with broad-spectrum sunscreen — TXA’s brightening benefits require UV protection for optimal results.

TXA, kojic acid, and α-arbutin target different control points in melanogenesis — they are complementary, not competitive. Kojic Acid works downstream by chelating copper at the tyrosinase active site; fastest initial visible brightening (4–8 weeks) but 12–63% contact sensitization risk and oxidative yellowing in formulations — best used at night with antioxidants. Alpha Arbutin is a slow-release competitive tyrosinase inhibitor; gentlest, most photostable option (pH 3.5–6.5), ideal for sensitive skin and daily use, but slower to show results (6–12 weeks). Tranexamic Acid (TXA) is unique — it blocks the upstream plasmin activation signal that neither kojic acid nor α-arbutin addresses, effectively stopping the melanogenesis “overproduction command” before tyrosinase activates. TXA = 50× vitamin C potency, strongest clinical evidence for melasma (28 RCTs), negligible irritation risk, and pH stable 4–8. Optimal formulation strategy: TXA (plasmin blockade) + α-Arbutin (tyrosinase inhibition) + Niacinamide (melanosome transfer inhibition) = three-pathway comprehensive brightening with zero cytotoxicity. Unlike hydroquinone, all three are globally compliant and safe for long-term use.

Every shipment includes: COA (HPLC purity ≥99.0% pharma or ≥98.0% cosmetic, full impurity profile, heavy metals ≤10 ppm with Pb ≤2 ppm / As ≤1 ppm / Hg ≤1 ppm / Cd ≤1 ppm, residual solvents per USP <467> / EP <5.4> / ICH Q3C, microbial panel per USP <61>/<62> and EP <2.6.12>/<2.6.13>), MSDS, HPLC Chromatogram (signed and dated), USP/EP Monograph Compliance Certificate (pharma grade), Type II DMF Support (pharma grade, with Letter of Authorization), BSE/TSE-Free Statement, Non-GMO Statement, Allergen Statement, HALAL Certificate, KOSHER Certificate, ISO 22000 + HACCP, ISO 9001:2015, FDA Facility Registration, Stability Data (25°C/60%RH real-time 36-month and 40°C/75%RH accelerated 6-month), and Complete Lot Traceability from raw material to finished product. Free sample available for qualified B2B buyers. MOQ: 1 kg. All documents provided in English. DMF Letter of Authorization available upon signed Confidentiality Agreement.