R-268712

Name: R-268712
Brand: MedChemExpress
SKU: HY-12953
Rating: 4.5 (1 reviews)

Cat. No.: HY-12953 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC₅₀ of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC₅₀ of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.

For research use only. We do not sell to patients.

R-268712 Chemical Structure

CAS No. : 879487-87-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 510	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

TGFBR1

2.5 nM (IC₅₀)

Smad3

10.4 nM (IC₅₀)

In Vitro

R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC₅₀ of 10.4 nM in HFL-1 cells^[1]. R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HFL-1 cells
Concentration:	3, 10, 30, 100, 300 nM
Incubation Time:	1 or 72 h
Result:	Inhibited the phosphorylation of Smad3 in a dose-dependent manner with an IC₅₀ of 10.4 nM when incubation 1 h. Suppressed myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth when incubation after 72 h.

In Vivo

R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC_0-24 values of 0.075, 0.28, 1.6 and 8.2 μg•h/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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male WKY/Hos rats^[2].

Dosage:

0.3, 1, 3, and 10 mg/kg

Administration:

Oral administration; single.

Result:

1.19 Pharmacokinetic 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)
AUC_0-24 (µg•h/mL)	0.075	0.28	1.6	8.2

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.

Molecular Weight

363.39

Formula

C₂₀H₁₈FN₅O

CAS No.

879487-87-3

Appearance

Solid

Color

White to light yellow

SMILES

FC1=C(C2=CN(CCO)N=C2)C=C(C3=CNN=C3C4=CC=CC(C)=N4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (343.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7519 mL	13.7593 mL	27.5186 mL
5 mM	0.5504 mL	2.7519 mL	5.5037 mL
10 mM	0.2752 mL	1.3759 mL	2.7519 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Terashima H, et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38. [Content Brief]

[2]. Terashima H, et al. 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. [Content Brief]

[3]. Wang H, et al. Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. Eur J Med Chem. 2020 Apr 1;191:112154. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7519 mL	13.7593 mL	27.5186 mL	68.7966 mL
	5 mM	0.5504 mL	2.7519 mL	5.5037 mL	13.7593 mL
	10 mM	0.2752 mL	1.3759 mL	2.7519 mL	6.8797 mL
	15 mM	0.1835 mL	0.9173 mL	1.8346 mL	4.5864 mL
	20 mM	0.1376 mL	0.6880 mL	1.3759 mL	3.4398 mL
	25 mM	0.1101 mL	0.5504 mL	1.1007 mL	2.7519 mL
	30 mM	0.0917 mL	0.4586 mL	0.9173 mL	2.2932 mL
	40 mM	0.0688 mL	0.3440 mL	0.6880 mL	1.7199 mL
	50 mM	0.0550 mL	0.2752 mL	0.5504 mL	1.3759 mL
	60 mM	0.0459 mL	0.2293 mL	0.4586 mL	1.1466 mL
	80 mM	0.0344 mL	0.1720 mL	0.3440 mL	0.8600 mL
	100 mM	0.0275 mL	0.1376 mL	0.2752 mL	0.6880 mL

R-268712 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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R-268712

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R-268712 Related Antibodies

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Complete Stock Solution Preparation Table

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