Asivatrep (Synonyms: PAC-14028) |
Catalog No.GC35407
One-Click Copy Product Info
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Asivatrep is a potent, selective, and nonsteroidal antagonist transient receptor potential vanilloid subfamily V member 1 (TRPV1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1005168-10-4
Sample solution is provided at 25 µL, 10mM.
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Asivatrep is a potent, selective, and nonsteroidal antagonist transient receptor potential vanilloid subfamily V member 1 (TRPV1) [1]. Asivatrep works by enhancing the production of key markers involved in skin differentiation, such as loricrin, filaggrin, involucrin, and certain keratins, leading to a reduction in dermatitis and pruritis[2]. Asivatrep has been widely used in various animal models to alleviate mild to moderate atopic dermatitis (AD)[3].
In vitro, Asivatrep (22.4μM) treatment for 48 hours downregulated the production of itch-related cytokines and decreased the phosphorylation level of NF-κB signaling factors in HaCaT cells[4].
In vivo, Asivatrep treatment via oral administration at a dose of 30mg/kg/day for three days significantly reduced skin itching in NC/Nga mice exposed to Dermatophagoides farina (Df) extract, alleviated mast cell degranulation, and decreased the level of IgG2a[5]. For consecutive 16 days, oral administration of 30mg/kg dose of Asivatrep daily notably inhibited the increase in trans-epidermal water loss (TEWL) in AD model mice induced by oxazolone (OXZ), and alleviated skin barrier damage[6]. For 11 consecutive days, applying 50μl of 1.0% Asivatrep cream twice daily significantly improved the skin inflammation in hairless mice induced by OXZ, reduced the thickening of the epidermis of the skin damage, and restored the barrier function of the stratum corneum[7].
References:
[1] Park C W, Kim B J, Lee Y W, et al. Asivatrep, a TRPV1 antagonist, for the topical treatment of atopic dermatitis: Phase 3, randomized, vehicle-controlled study (CAPTAIN-AD)[J]. Journal of Allergy and Clinical Immunology, 2022, 149(4): 1340-1347. e4.
[2] Shergill M, Bajwa B, Yilmaz O, et al. Biologic and small molecule therapy in atopic dermatitis[J]. Biomedicines, 2024, 12(8): 1841.
[3] Choi J K, Cho W, Lee J H, et al. A TRPV1 antagonist, PAC-14028 does not increase the risk of tumorigenesis in chemically induced mouse skin carcinogenesis[J]. Regulatory Toxicology and Pharmacology, 2020, 112: 104613.
[4] Yoon J H, Woo B Y, Kim M Y, et al. Attenuation of senile pruritus by PAC-14028-mediated downregulation of the NF-κB and MAPK pathways[J]. International Journal of Immunopathology and Pharmacology, 2025, 39: 03946320251321354.
[5] Yun J W, Seo J A, Jang W H, et al. Antipruritic effects of TRPV1 antagonist in murine atopic dermatitis and itching models[J]. Journal of investigative dermatology, 2011, 131(7): 1576-1579.
[6] Yun J W, Seo J A, Jeong Y S, et al. TRPV1 antagonist can suppress the atopic dermatitis-like symptoms by accelerating skin barrier recovery[J]. Journal of dermatological science, 2011, 62(1): 8-15.
[7] Lee J H, Choi C S, Bae I H, et al. A novel, topical, nonsteroidal, TRPV1 antagonist, PAC-14028 cream improves skin barrier function and exerts anti-inflammatory action through modulating epidermal differentiation markers and suppressing Th2 cytokines in atopic dermatitis[J]. Journal of Dermatological Science, 2018, 91(2): 184-194.
| Cell experiment [1]: | |
Cell lines | HaCaT cells |
Preparation Method | HaCaT cells were seeded at a density of 4×105 cells per well in a 6-well plate. Cells were cultured in DMEM medium containing 10% fetal bovine serum and 1% penicillin-streptomycin in a 5% CO2 incubator overnight. Subsequently, the cells were incubated with different concentrations of Asivatrep (0, 5.6, 11.2, 22.4µM) for 2 hours, followed by incubation with 20nM IL-17A for 2 hours. The expression of TRPV1 and inflammatory factors was then analyzed. |
Reaction Conditions | 0, 5.6, 11.2, 22.4µM; 2h |
Applications | Asivatrep treatment reduced TRPV1, IL-4, and IL-13 mRNA expression in HaCaT cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female hairless mice |
Preparation Method | Female hairless mice (7 weeks old) were raised in a controlled environment (23±3°C, relative humidity 40–60%, 12/12 light-dark cycle), with ad free access to laboratory feed and tap water. On day 0, 50μl of 5% OXZ solution was applied to the neck of the hairless mice for sensitization, and then 100μl of 0.1% OXZ solution was applied to both sides of the mice every day for 15 days. From the day before the first OXZ sensitization to the day of sacrifice, mice were given Asivatrep (30mg/kg/day; p.o.) every day for 16 days. After the treatment, the TEWL on the back of the mice, the thickness of skin inflammation, and the severity of AD-like symptoms were measured. |
Dosage form | 30mg/kg/day for 16 days; p.o. |
Applications | Asivatrep inhibited the increase in TEWL in AD model mice, and alleviated the general AD-like symptoms, including serum IgE increase, mast cell degranulation, scratching behavior and clinical severity of dermatitis. |
References: | |
| Cas No. | 1005168-10-4 | SDF | |
| Synonyms | PAC-14028 | ||
| Canonical SMILES | O=C(N[C@@H](C1=CC(F)=C(NS(=O)(C)=O)C(F)=C1)C)/C=C/C2=CC=C(C(F)(F)F)N=C2CCC | ||
| Formula | C21H22F5N3O3S | M.Wt | 491.47 |
| Solubility | DMSO: 50 mg/mL (101.74 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0347 mL | 10.1736 mL | 20.3471 mL |
| 5 mM | 406.9 μL | 2.0347 mL | 4.0694 mL |
| 10 mM | 203.5 μL | 1.0174 mL | 2.0347 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)