| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 25mg | |||
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| Targets |
Asivatrep targets the transient receptor potential vanilloid type I (TRPV1) receptor. TRPV1 is a non-selective cation channel expressed on sensory neurons that is activated by noxious heat, protons, and capsaicin, playing a key role in pain and itch perception. As a TRPV1 antagonist, Asivatrep blocks the receptor, thereby reducing neuronal excitability and alleviating itch and inflammatory pain.
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| 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].
In vitro, Asivatrep (PAC-14028) demonstrates potent and selective antagonism of the TRPV1 receptor. It effectively blocks capsaicin- or acid-induced calcium influx in TRPV1-expressing cells. The compound shows high selectivity for TRPV1 over other transient receptor potential channels and has been characterized for its ability to suppress pruritus and inflammatory responses in cellular models of atopic dermatitis and acne. |
| 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].
In vivo, Asivatrep has demonstrated efficacy against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain. It prevents barrier damage, accelerates skin barrier recovery, and suppresses pruritus, showing potential for the treatment of atopic dermatitis. The compound has also been evaluated in models of acne and has shown anti-inflammatory effects. |
| Enzyme Assay |
Specific cell-free binding assay protocols for Asivatrep involve radioligand binding assays using membranes expressing recombinant TRPV1 receptors. Competitive displacement of a radiolabeled TRPV1 ligand (such as [³H]resiniferatoxin) is measured to determine binding affinity. The compound's antagonist activity is confirmed in cell-free systems by assessing its ability to inhibit capsaicin-induced channel opening using fluorescent membrane potential assays.
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| Cell Assay |
In vitro cell-based assays for Asivatrep use cell lines expressing recombinant human TRPV1 receptors (such as HEK293-TRPV1 cells). Cells are loaded with calcium-sensitive fluorescent dyes (e.g., Fluo-4), and TRPV1 activation is induced by capsaicin or acid. Asivatrep's inhibition of calcium influx is measured fluorometrically to determine IC50 values. The compound's effects on inflammatory cytokine production are assessed in keratinocyte or immune cell cultures.
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| Animal Protocol |
In vivo animal studies for Asivatrep have been conducted in various disease models. In models of atopic dermatitis, the compound is typically administered topically or orally to assess its effects on skin barrier function, pruritus, and inflammation. In inflammatory pain models, Asivatrep is evaluated for its analgesic effects. Disease models include visceral pain, inflammatory bowel disease, and inflammatory pain.
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| ADME/Pharmacokinetics |
Asivatrep shows a plasma half-life of 2.1 hours in rats and 3.8 hours in minipigs. The compound has a molecular weight of 503.50 g/mol and a molecular formula of C23H24F4N4O3S. It is soluble in DMSO and appears as a solid powder. The compound's pharmacokinetic properties support its development as a topical or systemic therapeutic agent.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Asivatrep are not extensively detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications without proper regulatory approval. As a TRPV1 antagonist, potential toxicities may include effects on thermoregulation and pain perception, though formal toxicological profiles are not extensively reported.
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| References |
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| Additional Infomation |
PAC-14028 has been used in research trials to treat pruritus, papulopustular rosacea, and erythematous telangiectasia rosacea.
Asivatrep (PAC-14028) is a potent and selective TRPV1 antagonist developed for the treatment of pruritus, atopic dermatitis, and acne. It has shown efficacy in preventing barrier damage and suppressing pruritus. The compound demonstrates activity against visceral pain, inflammatory bowel disease, and inflammatory pain. No clinical trial or approved indication data are available in the provided sources. |
| 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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