| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
hTRPV1 2.66 nM (IC50) TRPM8 7.45 μM (IC50)
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|---|---|
| ln Vitro |
Compared to other TRP channels, TRPV1 antagonist 3 (Compound 7q) has a high degree of selectivity for the TRPV1 receptor[1]. TRPV1 antagonist 3 exhibits a satisfactory solubility in water (26 μg/mL at pH 7.4) [1].
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| ln Vivo |
The anti-nociceptive effect of TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; ip; 30 min) is mostly mediated by inhibiting CAP-activated channel[1]. In rats, the TRPV1 antagonist 3 (0-100 mg/kg; ig) exhibited no discernible thermal effect[1]. TRPV1 antagonist 3 (10 mg/kg; iv) has good CNS penetration, with a brain/plasma ratio of 1.66, and a decent concentration in the brain at 0.5 hours, with a value of 2311 ng/g[1].
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| Animal Protocol |
Animal/Disease Models: KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1]
Doses: 3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected sc under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse ip). Route of Administration: intraperitoneally (ip) administration; 30 min Experimental Results: In capsaicin-induced nociception, licking time diminished Dramatically in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg. Animal/Disease Models: Spragur-Dawley male rats (220-250 g)[1] Doses: 10 mg/kg or 20 mg /kg Route of Administration: intravenous (iv) injection of 10 mg/kg or oral dose of 20 mg/kg (pharmacokinetic/PK Analysis) Experimental Results: In vivo pharmacokinetic/PK parameters of TRPV1 antagonist 3 in rats (n=3)[1 |
| References |
| Molecular Formula |
C23H25N3OS
|
|---|---|
| Molecular Weight |
391.52910399437
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| Exact Mass |
391.171
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| CAS # |
2765294-54-8
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| PubChem CID |
163322232
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| Appearance |
Off-white to pale purple solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
522
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)C1=CC(=CC=C1)NC(=O)N2CCC[C@H]2C3=NC=C(S3)C4=CC=CC=C4
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| InChi Key |
CZISSZWUQQBGMU-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C23H25N3OS/c1-16(2)18-10-6-11-19(14-18)25-23(27)26-13-7-12-20(26)22-24-15-21(28-22)17-8-4-3-5-9-17/h3-6,8-11,14-16,20H,7,12-13H2,1-2H3,(H,25,27)/t20-/m0/s1
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| Chemical Name |
(2S)-2-(5-phenyl-1,3-thiazol-2-yl)-N-(3-propan-2-ylphenyl)pyrrolidine-1-carboxamide
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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: ≥ 100 mg/mL (255.41 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5541 mL | 12.7704 mL | 25.5408 mL | |
| 5 mM | 0.5108 mL | 2.5541 mL | 5.1082 mL | |
| 10 mM | 0.2554 mL | 1.2770 mL | 2.5541 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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