SB-705498
- CAS No.
- 501951-42-4
- Chemical Name:
- SB-705498
- Synonyms
- CS-279;SB-705498;SB 705498;SB705498;SB-705498, 10 mM in DMSO;1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)-2-pyridyl]pyrrolidin-3-yl]urea;(R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea;1-(2-Bromophenyl)-3-{(3S)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl}urea;N-(2-Bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]urea;Urea, N-(2-bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]-
- CBNumber:
- CB22628383
- Molecular Formula:
- C17H16BrF3N4O
- Molecular Weight:
- 429.23
- MDL Number:
- MFCD13152399
- MOL File:
- 501951-42-4.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| SB-705498 ≥98% | 17313 | 1mg | $43 |
| SB-705498 ≥98% | 17313 | 5mg | $76 |
| SB-705498 ≥98% | 17313 | 10mg | $129 |
| SB-705498 ≥98% | 17313 | 1mg | $39 |
| SB-705498 ≥98% | 17313 | 5mg | $69 |
| More product size | |||
| Boiling point | 506.9±50.0 °C(Predicted) |
|---|---|
| Density | 1.59 |
| storage temp. | -20°C |
| solubility | Soluble in DMSO (>25 mg/ml) |
| pka | 13.00±0.20(Predicted) |
| form | solid |
| color | White |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| InChI | InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-5-11(9-22-15)17(19,20)21/h1-6,9,12H,7-8,10H2,(H2,23,24,26)/t12-/m1/s1 |
| InChIKey | JYILLRHXRVTRSH-GFCCVEGCSA-N |
| SMILES | N(C1=CC=CC=C1Br)C(N[C@@H]1CCN(C2=NC=C(C(F)(F)F)C=C2)C1)=O |
| FDA UNII | T74V9O0Y2W |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405 | |||||||||
| NFPA 704 |
|
SB-705498 price More Price(54)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17313 | SB-705498 ≥98% | 501951-42-4 | 1mg | $43 | 2026-04-30 | Buy |
| Cayman Chemical | 17313 | SB-705498 ≥98% | 501951-42-4 | 5mg | $76 | 2026-04-30 | Buy |
| Cayman Chemical | 17313 | SB-705498 ≥98% | 501951-42-4 | 10mg | $129 | 2026-04-30 | Buy |
| Cayman Chemical | 17313 | SB-705498 ≥98% | 501951-42-4 | 1mg | $39 | 2024-03-01 | Buy |
| Cayman Chemical | 17313 | SB-705498 ≥98% | 501951-42-4 | 5mg | $69 | 2024-03-01 | Buy |
SB-705498 Chemical Properties,Uses,Production
Description
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin . SB-705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated activation of TRPV1 receptors (pKis = 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively). It has been shown to induce rapid, reversible inhibition of capsaicin (IC50 = 3 nM)-, acid (pH 5.3)-, or heat (50°C; IC50 = 6 nM)-mediated activation of human TRPV1 (at -70 mV).
Uses
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
in vitro
using a ca2+-based fluorometric imaging plate reader (flipr) assay, sb-705498 was shown to be a potent competitive antagonist of the capsaicin-mediated activation of the human trpv1 receptor (pki = 7.6) with activity at rat (pki = 7.5) and guinea pig (pki = 7.3) orthologs. sb-705498 caused rapid and reversible inhibition of the capsaicin (ic50 = 3 nm)-, acid (ph 5.3)-, or heat (50°c; ic50 = 6 nm)-mediated activation of human trpv1 (at =70 mv) [1].
in vivo
having initially demonstrated that sb-705498 showed good overall in vitro efficacy and oral bioavailability in rat, the in vivo activity of sb-705498 was investigated in the capsaicin-induced secondary hyperalgesia model9 in the rat. this model demonstrates the compound’s antagonist activity in vivo against the specific trpv1 agonist capsaicin. as an early indicator of potential pharmacodynamic activity, sb-705498 showed excellent activity at 10 and 30 mg/kg po with good reversal of allodynia. furthermore, sb-705498 was also shown to give 80% reversal of allodynia in the guinea pig fca model at 10 mg/kg po [2].
target
hTRPV1
References
[1] HARSHAD K. RAMI et al. et al. Discovery of SB-705498: A Potent, Selective and Orally Bioavailable TRPV1 Antagonist Suitable for Clinical Development.[J]. ChemInform, 2006, 37 38. DOI:10.1002/chin.200638200
[2] MARTIN J GUNTHORPE. Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 321 3: 1183-1192. DOI:10.1124/jpet.106.116657
SB-705498 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Shaanxi Dideu Medichem Co. Ltd | +86-29-87569266 +86-17392581500 | 1015@dideu.com | China | 3861 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32468 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +86-13203830695 | laboratory@coreychem.com | China | 30224 | 58 |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19853 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10457 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9984 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39037 | 58 |
| Aceschem Inc. | +1-817863-6948 +1-（817）863-6948 | sales@aceschem.com | United States | 19632 | 58 |
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