R-268712 | CAS#879487-87-3 | ALK5 inhibitor

MedKoo Cat#: 562919 | Name: R-268712

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

R-268712 is a specific inhibitor of activin receptor-like kinase 5 (ALK5). It is also an orally active transforming growth factor-β type I receptor inhibitor.

Chemical Structure

R-268712

CAS#879487-87-3

Theoretical Analysis

MedKoo Cat#: 562919

Name: R-268712

CAS#: 879487-87-3

Chemical Formula: C20H18FN5O

Exact Mass: 363.1495

Molecular Weight: 363.39

Elemental Analysis: C, 66.10; H, 4.99; F, 5.23; N, 19.27; O, 4.40

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 525.00	2 Weeks
250mg	USD 975.00	2 Weeks

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Related CAS #

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Synonym

R-268712; R 268712; R268712;

IUPAC/Chemical Name

2-[4-[2-Fluoro-5-[3-(6-methylpyridine-2-yl)-1H-pyrazol-4-yl] phenyl] pyrazol-1-yl]ethanol

InChi Key

JQGOCCALXFSRHZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H18FN5O/c1-13-3-2-4-19(24-13)20-17(11-22-25-20)14-5-6-18(21)16(9-14)15-10-23-26(12-15)7-8-27/h2-6,9-12,27H,7-8H2,1H3,(H,22,25)

SMILES Code

CC1=CC=CC(C2=NNC=C2C3=CC=C(F)C(C4=CN(CCO)N=C4)=C3)=N1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and ethanol

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

R-268712 is a potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). It suppresses development of renal fibrosis in a unilateral ureteral obstruction model. R 268712 also reduces proteinuria, glomerulosclerosis and improves renal function in an anti-Thy1 glomerulonephritis model. Orally bioavailable.

In vitro activity:

This study suggests that R-268712 and other ALK5 inhibitors could suppress glomerulonephritis as well as glomerulosclerosis by an inhibitory mechanism that involves suppression of TGF-β signaling. Reference: Eur J Pharmacol. 2014 Jul 5;734:60-6. https://pubmed.ncbi.nlm.nih.gov/24726873/

In vivo activity:

R-268712-was effective in inhibiting luciferase activity in both the in vivo bleomycin-induced lung fibrosis model and in vitro primary mouse lung fibroblasts. Reference: Pulm Pharmacol Ther. 2019 Feb;54:31-38. https://pubmed.ncbi.nlm.nih.gov/30448291/

	Solvent	mg/mL	mM
Solubility
	Ethanol	18.2	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 363.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Terashima H, Kato M, Ebisawa M, Kobayashi H, Suzuki K, Nezu Y, Sada T. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6. doi: 10.1016/j.ejphar.2014.03.045. Epub 2014 Apr 12. PMID: 24726873. 2. Terashima H, Aonuma M, Tsuchida H, Sugimoto K, Yokoyama M, Kato M. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38. doi: 10.1016/j.pupt.2018.11.005. Epub 2018 Nov 15. PMID: 30448291.

In vitro protocol:

In vivo protocol:

1. Terashima H, Aonuma M, Tsuchida H, Sugimoto K, Yokoyama M, Kato M. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38. doi: 10.1016/j.pupt.2018.11.005. Epub 2018 Nov 15. PMID: 30448291.

1: Terashima H, Kato M, Ebisawa M, Kobayashi H, Suzuki K, Nezu Y, Sada T. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6. doi: 10.1016/j.ejphar.2014.03.045. Epub 2014 Apr 12. PubMed PMID: 24726873.