LDN-193188 | CAS#1267610-30-9 | PC-TP inhibitor

MedKoo Cat#: 563574 | Name: LDN-193188

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Description:

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

LDN-193188 is a inhibitor of phosphatidylcholine transfer protein (PC-TP).

Chemical Structure

LDN-193188

CAS#1267610-30-9

Theoretical Analysis

MedKoo Cat#: 563574

Name: LDN-193188

CAS#: 1267610-30-9

Chemical Formula: C20H17Cl2N5O4S

Exact Mass: 493.0378

Molecular Weight: 494.35

Elemental Analysis: C, 48.59; H, 3.47; Cl, 14.34; N, 14.17; O, 12.95; S, 6.49

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 365.00	2 Weeks

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Related CAS #

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Synonym

LDN-193188; LDN 193188; LDN193188;

IUPAC/Chemical Name

2,4-Dichloro-N-[[[4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl]-amino]carbonyl]benzamide

InChi Key

COTBDKMEUUNJTI-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H17Cl2N5O4S/c1-11-9-12(2)24-19(23-11)27-32(30,31)15-6-4-14(5-7-15)25-20(29)26-18(28)16-8-3-13(21)10-17(16)22/h3-10H,1-2H3,(H,23,24,27)(H2,25,26,28,29)

SMILES Code

O=C(NC(NC1=CC=C(S(=O)(NC2=NC(C)=CC(C)=N2)=O)C=C1)=O)C3=CC=C(Cl)C=C3Cl

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

Shelf Life

>3 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

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

LDN 193188 is an inhibitor of phosphatidylcholine transfer protein (PC-TP).

In vitro activity:

One of these (LDN-0028202), was not sufficiently soluble to characterize reproducibly, but a close analogue (LDN-0193188) proved to be both soluble and effective as a PC-TP inhibitor, as demonstrated by Figure 5. Reference: Anal Biochem. 2008 Dec 1;383(1):85-92. https://pubmed.ncbi.nlm.nih.gov/18762160/

In vivo activity:

Treatment with compound A1 (LDN-193188) led to a 31% reduction in fasting plasma glucose concentrations (mg/dl) in wild type mice, but did not significantly affect Pctp−/− mice (Table 1). The inhibitor improved glucose tolerance tests for wild type mice (Fig. 4A), as evidenced by separation of the response curves and a 20% reduction in AUC compared with vehicle-treated controls. Reference: Hepatology. 2011 Aug;54(2):664-74. https://pubmed.ncbi.nlm.nih.gov/21538437/

	Solvent	mg/mL	mM
Solubility
	DMSO	49.4	100.00

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 494.35 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. Shishova EY, Stoll JM, Ersoy BA, Shrestha S, Scapa EF, Li Y, Niepel MW, Su Y, Jelicks LA, Stahl GL, Glicksman MA, Gutierrez-Juarez R, Cuny GD, Cohen DE. Genetic ablation or chemical inhibition of phosphatidylcholine transfer protein attenuates diet-induced hepatic glucose production. Hepatology. 2011 Aug;54(2):664-74. doi: 10.1002/hep.24393. Epub 2011 Jun 23. PMID: 21538437; PMCID: PMC3144994. 2. Wagle N, Xian J, Shishova EY, Wei J, Glicksman MA, Cuny GD, Stein RL, Cohen DE. Small-molecule inhibitors of phosphatidylcholine transfer protein/StarD2 identified by high-throughput screening. Anal Biochem. 2008 Dec 1;383(1):85-92. doi: 10.1016/j.ab.2008.07.039. Epub 2008 Aug 12. PMID: 18762160; PMCID: PMC2783649.

In vitro protocol:

In vivo protocol:

1: Shishova EY, Stoll JM, Ersoy BA, Shrestha S, Scapa EF, Li Y, Niepel MW, Su Y, Jelicks LA, Stahl GL, Glicksman MA, Gutierrez-Juarez R, Cuny GD, Cohen DE. Genetic ablation or chemical inhibition of phosphatidylcholine transfer protein attenuates diet-induced hepatic glucose production. Hepatology. 2011 Aug;54(2):664-74. doi: 10.1002/hep.24393. Epub 2011 Jun 23. PubMed PMID: 21538437; PubMed Central PMCID: PMC3144994.