ChemicalBook > CAS DataBase List > SB-705498

SB-705498

Product Name
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
Formula Weight
429.23
MOL File
501951-42-4.mol
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SB-705498 Property

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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
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N-Bromosuccinimide Price

Cayman Chemical
Product number
17313
Product name
SB-705498
Purity
≥98%
Packaging
1mg
Price
$39
Updated
2024/03/01
Cayman Chemical
Product number
17313
Product name
SB-705498
Purity
≥98%
Packaging
5mg
Price
$69
Updated
2024/03/01
Cayman Chemical
Product number
17313
Product name
SB-705498
Purity
≥98%
Packaging
10mg
Price
$117
Updated
2024/03/01
ChemScene
Product number
CS-0757
Product name
SB-705498
Purity
99.98%
Packaging
10mg
Price
$150
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
KIN0001083
Product name
SB-705498
Purity
95.00%
Packaging
1MG
Price
$165.9
Updated
2021/12/16
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SB-705498 Chemical Properties,Usage,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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SB-705498 Suppliers

China 86 India 1 United States 15 Global 102
MQ (shanghai) Pharmaceuticals Co., Ltd.
Tel
13761635123
Fax
1014988033@qq
Email
1014988033@qq.com
Country
China
ProdList
4969
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Tianjin Derchemist Science & Technology Co., Ltd.
Tel
22-58627059 13920586291
Fax
022-58620305
Email
zdcomcon@126.com
Country
China
ProdList
3401
Advantage
50
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Fax
0512-87182056
Email
lingling.qi@yacoo.com.cn
Country
China
ProdList
7295
Advantage
60
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58

501951-42-4, SB-705498Related Search:

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  • 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