[CAS NO. 193022-04-7] CTS-1027

Name: CTS-1027
Brand: Arctom Scientific
SKU: AS359452

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PRODUCTS SPECIFICATIONS [193022-04-7]

Distributor

Catalog

AS359452

Brand

Arctom Scientific

CAS

193022-04-7

DESCRIPTION [193022-04-7]

Overview

MDL	MFCD16657131
Molecular Weight	425.88
Molecular Formula	C19H20ClNO6S
SMILES	O=C(NO)C1(CCOCC1)CS(=O)(C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)=O

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

1 Publications Citing Use of MCE

[1]ACS Comb Sci. 2019 Dec 9;21(12):805-816.

Summary

CTS-1027 is a potent small molecule inhibitor of MMPs , with IC ₅₀ s of 0.3 nM, 0.5 nM for MMP2 , MMP13 , respectively, and has > 1,000 fold selectivity over MMP1.

IC50 & Target

IC50: 0.2 nM (MMP2), 0.5 nM (MMP13), 0.7 nM (MMP12), 0.9 nM (MMP8), 9.5 nM (MMP3), 15 nM (MMP14)

In Vivo

CTS-1027 significantly reduces the hepatocyte apoptosis, features of cholestatic liver injury, amd markers of hepatic fibrogenesis in the BDL mouse. CTS-1027 improves overall animal survival following 14 days of BDL in mice ^[1] . In male animals treated for 8 weeks the terminal plasma concentration of RS-130830 is 311±45 nM. Treatment of male mice with RS-130830 for 8 weeks causes an 89% increase in plasma triglyceride concentration, but there is no corresponding effect in female mice treated for 12 weeks. The plaque lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01051921	Conatus Pharmaceuticals Inc.	Hepatitis C	January 2010	Phase 2
NCT01273064	Conatus Pharmaceuticals Inc.	Hepatitis C	January 2011	Phase 2
NCT00925990	Conatus Pharmaceuticals Inc.	Hepatitis C	June 2009	Phase 2
NCT00570336	Conatus Pharmaceuticals Inc.\|FGK Clinical Research GmbH	Chronic Hepatitis C Virus Infection	December 2007	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 234.81 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3481 mL	11.7404 mL	23.4808 mL
5 mM	0.4696 mL	2.3481 mL	4.6962 mL
10 mM	0.2348 mL	1.1740 mL	2.3481 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

* All of the co-solvents are available by MCE.