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R-268712

Product Name
R-268712
CAS No.
879487-87-3
Chemical Name
R-268712
Synonyms
2025;R-268712;CID 11703284;R-268712 ，S7710;R 268712;R268712;R-268712, 10 mM in DMSO;4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol;1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-;2-(4-(2-fluoro-5-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)phenyl)-1H-pyrazol-1-yl)ethanol;2-(4-(2-Fluoro-5-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)phenyl)-1H-pyrazol-1-yl)ethan-1-ol
CBNumber
CB53126704
Molecular Formula
C20H18FN5O
Formula Weight
363.39
MOL File
879487-87-3.mol
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R-268712 Property

Boiling point:
576.8±50.0 °C(Predicted)
Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
DMSO : 125 mg/mL (343.98 mM)
pka
10.96±0.50(Predicted)
form 
Solid
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
36810
Product name
R-268712
Purity
≥98%
Packaging
5mg
Price
$29
Updated
2026/04/30
Cayman Chemical
Product number
36810
Product name
R-268712
Purity
≥98%
Packaging
10mg
Price
$51
Updated
2026/04/30
Cayman Chemical
Product number
36810
Product name
R-268712
Purity
≥98%
Packaging
50mg
Price
$169
Updated
2026/04/30
Cayman Chemical
Product number
36810
Product name
R-268712
Purity
≥98%
Packaging
100mg
Price
$253
Updated
2026/04/30
Tocris
Product number
5288
Product name
R268712
Purity
≥98%(HPLC)
Packaging
10
Price
$270
Updated
2021/12/16
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R-268712 Chemical Properties,Usage,Production

Uses

R 268712 is an orally active transforming growth factor-β type I receptor inhibitor, which prevents glomerular sclerosis in a Thy1 nephritis model.

in vivo

R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC0-24 values of 0.075, 0.28, 1.6 and 8.2 μgh/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively[2].
R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model[2].
R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg[2].

Animal Model:Male WKY/Hos rats[2].
Dosage:0.3, 1, 3, and 10 mg/kg
Administration:Oral administration; single.
Result:1.19Pharmacokinetic Parameters of R-268712 in male WKY/Hos rats (n=4)[2].
PO (0.3 mg/kg)PO (1 mg/kg)PO (3 mg/kg)PO (10 mg/kg)
AUC0-24 (μgh/mL)0.0750.281.68.2
Animal Model:Male Col1a1-Luc Tg rats (10 to14-week-old; UUO model; n=5-6)[2].
Dosage:1, 3, 10 mg/kg
Administration:Oral administration; single daily for 3 days.
Result:Suppressed activity of renal luciferase in a dose-dependent manner.
Animal Model:Male WKY/Hos rats (4-week-old; Thy1 nephritis model; n=7)[2].
Dosage:0.3, 1 mg/kg
Administration:Oral administration; single daily for 33 days.
Result:Significantly reduced proteinuria at day 21( the repression continued until day 28), and serum creatinine level (dosage at 1 mg/kg).
Apparently suppressed glomerular sclerosis by 28% and reduced the increase of the hydroxyproline content when at 1 mg/kg.
Suppressed the activation of mesangial parenchymal cell and the injury of podocyte on the basis of TGF-β signaling inhibition at 1 mg/kg.

IC 50

TGFBR1: 2.5 nM (IC50); Smad3: 10.4 nM (IC50)

storage

Store at -20°C

R-268712 Preparation Products And Raw materials

Raw materials

Preparation Products

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R-268712 Suppliers

China 53 United Kingdom 1 United States 6 Global 60
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13770331960
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
16059
Advantage
64
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
26707
Advantage
65
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
39999
Advantage
60
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7777
Advantage
56
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4827
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
89689
Advantage
60
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2987
Advantage
58
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9550
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
0-2022843681 15618226720
Fax
+86-21-51601218
Email
chaolaichem@foxmail.com
Country
China
ProdList
9955
Advantage
58

879487-87-3, R-268712Related Search:


  • R-268712
  • 2025
  • R 268712;R268712
  • 4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol
  • 1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-
  • 2-(4-(2-Fluoro-5-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)phenyl)-1H-pyrazol-1-yl)ethan-1-ol
  • renal fibrosis,Thy1 nephritis,Transforming growth factor beta receptors,glomerulonephritis,Transforming growth factor beta,ALK tyrosine kinase receptor,HFL-1,R 268712,glomerulosclerosis,CD246,Inhibitor,Cluster of differentiation 246,UUO,Anaplastic lymphoma kinase (ALK),R268712,inhibit,TGF-β,TGF-beta/Smad,CKD,R-268712,TGF-β Receptor,Anaplastic lymphoma kinase
  • 2-(4-(2-fluoro-5-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)phenyl)-1H-pyrazol-1-yl)ethanol
  • CID 11703284
  • R-268712, 10 mM in DMSO
  • 2-(4-(2-Fluoro-5-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)phenyl)-1H-pyrazol-1-yl)ethan-1-ol?,R-268712
  • R-268712 ，S7710
  • 879487-87-3