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SB-705498

CAS No.
501951-42-4
Chemical Name:
SB-705498
Synonyms
CS-279;SB-705498;SB 705498;SB705498;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;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
Last updated:2023-09-04 16:42:00

SB-705498 Properties

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.
FDA UNII T74V9O0Y2W

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
NFPA 704
0
2 0

SB-705498 price More Price(16)

Manufacturer Product number Product description CAS number Packaging Price Updated 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
Cayman Chemical 17313 SB-705498 ≥98% 501951-42-4 10mg $117 2024-03-01 Buy
ChemScene CS-0757 SB-705498 99.98% 501951-42-4 10mg $150 2021-12-16 Buy
American Custom Chemicals Corporation KIN0001083 SB-705498 95.00% 501951-42-4 1MG $165.9 2021-12-16 Buy
Product number Packaging Price Buy
17313 1mg $39 Buy
17313 5mg $69 Buy
17313 10mg $117 Buy
CS-0757 10mg $150 Buy
KIN0001083 1MG $165.9 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).

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

Rami et al. (2006), ?Discovery of SB-705498: a potent and orally bioavailable TRPV1 antagonist suitable for clinical development; Bioorg. Med. Chem. Lett., 16 3287 Gunthorpe et al. (2007), 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. Pharmacol. Exp. Ther., 321 1183

SB-705498 Preparation Products And Raw materials

Raw materials

Preparation Products

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ATK CHEMICAL COMPANY LIMITED
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Shanghai Acmec Biochemical Technology Co., Ltd.
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SB-705498 Spectrum

SB-705498 N-(2-Bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]urea (R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea 1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)-2-pyridyl]pyrrolidin-3-yl]urea CS-279 SB 705498;SB705498 Urea, N-(2-bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]- 501951-42-4 C17H16BrF3N4O Inhibitors