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Asivatrep (PAC 14028) is novel, potent and selective TRPV1 (transient receptor potential vanilloid type I) antagonist. It can be potentially used for the treatment of pruritus and acne
| ln Vitro |
Asivatrep (PAC-14028) has the potential to cure atopic dermatitis since it avoids barrier degradation, speeds up skin barrier healing, and reduces itching. It has the ability to suppress the rise in serum IgE, mast cell degranulation, and infiltration of epidermal inflammatory cells linked to atopic dermatitis [1]. Asivatrep (PAC-14028) has demonstrated effectiveness in a number of illness models, such as inflammatory pain, visceral pain, and inflammatory bowel disease [2].
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| ln Vivo |
Asivatrep's (PAC-14028) plasma half-life in rats was 2.1 hours, whereas in minipigs, it was somewhat longer at 3.8 hours. In rats and minipigs, the oral bioavailability of a 10 mg/kg dosage was 52.7% and 64.2%, respectively. These results suggest that Asivatrep (PAC-14028) is comparatively well absorbed when taken orally [1]. At submicromolar concentrations, asivatrep (PAC-14028) prevents the calcium influx in keratinocytes that is triggered by capsaicin. In vivo, this strong TRPV1 antagonistic activity in keratinocytes is demonstrated by blocking capsaicin-induced increases in blood perfusion and speeding up the healing of the damaged barrier caused by tape stripping in hairless mice [3].
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| References |
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| Additional Infomation |
PAC-14028 has been used in trials studying the treatment of Skin Pruritus, Papulopustular Rosacea, and Erythematotelangiectatic Rosacea.
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| Molecular Formula |
C21H22F5N3O3S
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|---|---|
| Molecular Weight |
491.4747
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| Exact Mass |
491.13
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| CAS # |
1005168-10-4
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| PubChem CID |
56649347
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.544
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| LogP |
3.71
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
775
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCC1=C(C=CC(=N1)C(F)(F)F)/C=C/C(=O)N[C@H](C)C2=CC(=C(C(=C2)F)NS(=O)(=O)C)F
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| InChi Key |
UKGJZDSUJSPAJL-YPUOHESYSA-N
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| InChi Code |
InChI=1S/C21H22F5N3O3S/c1-4-5-17-13(6-8-18(28-17)21(24,25)26)7-9-19(30)27-12(2)14-10-15(22)20(16(23)11-14)29-33(3,31)32/h6-12,29H,4-5H2,1-3H3,(H,27,30)/b9-7+/t12-/m1/s1
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| Chemical Name |
(R,E)-N-(1-(3,5-difluoro-4-(methylsulfonamido)phenyl)ethyl)-3-(2-propyl-6-(trifluoromethyl)pyridin-3-yl)acrylamide
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| Synonyms |
PAC 14028 PAC-14028 PAC14028 Asivatrep
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~101.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0347 mL | 10.1736 mL | 20.3471 mL | |
| 5 mM | 0.4069 mL | 2.0347 mL | 4.0694 mL | |
| 10 mM | 0.2035 mL | 1.0174 mL | 2.0347 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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