ChemicalBook > CAS DataBase List > GSK 2330672

GSK 2330672

Product Name: GSK 2330672
CAS No.: 1345982-69-5
Chemical Name: GSK 2330672
Synonyms: linerixibat;CS-2639;GSK 2330672;Iinerixibat;linerixibat (GSK2330672);GSK 2330672; GSK-2330672;Iinerixibat (GSK2330672);Linerixibat, 10 mM in DMSO;3-((((3R,5R)-3-Butyl-3-ethyl-7-methoxy-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepin-8-yl)methyl)amino)pentanedioic acid;Pentanedioic acid, 3-((((3R,5R)-3-butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl)methyl)amino)-
CBNumber: CB12716247
Molecular Formula: C28H38N2O7S
Formula Weight: 546.68
MOL File: 1345982-69-5.mol

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GSK 2330672 Property

Boiling point:: 730.8±60.0 °C(Predicted)
Density: 1.218±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF: 5 mg/ml; DMSO: 2 mg/ml; PBS (pH 7.2): 0.2 mg/ml
form: A crystalline solid
pka: 3.27±0.10(Predicted)
color: White to off-white
InChIKey: CZGVOBIGEBDYTP-VSGBNLITSA-N
SMILES: C(O)(=O)CC(NCC1C=C2S(=O)(=O)C[C@](CCCC)(CC)N[C@H](C3=CC=CC=C3)C2=CC=1OC)CC(O)=O

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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

H401Toxic to aquatic life

H411Toxic to aquatic life with long lasting effects

Precautionary statements

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

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

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

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P391Collect spillage. Hazardous to the aquatic environment

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23843
Product name: GSK2330672
Purity: ≥98%
Packaging: 1mg
Price: $110
Updated: 2024/03/01

Cayman Chemical

Product number: 23843
Product name: GSK2330672
Purity: ≥98%
Packaging: 5mg
Price: $515
Updated: 2024/03/01

Cayman Chemical

Product number: 23843
Product name: GSK2330672
Purity: ≥98%
Packaging: 10mg
Price: $918
Updated: 2024/03/01

AK Scientific

Product number: 4578DL
Product name: Linerixibat
Packaging: 5mg
Price: $671
Updated: 2021/12/16

Crysdot

Product number: CD31003808
Product name: GSK2330672
Purity: 98+%
Packaging: 5mg
Price: $208
Updated: 2021/12/16

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GSK 2330672 Chemical Properties,Usage,Production

Description

GSK2330672 is an inhibitor of the apical sodium-dependent bile acid transporter (ASBT; IC₅₀s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively). In vivo, GSK2330672 (0.05 mg/kg) stimulates fecal bile acid secretion, reduces hemoglobin A1c (HbA1c) and plasma glucose levels, and increases total GLP-1 and plasma insulin in Zucker diabetic fatty (ZDF) rats.

Uses

Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment[1][2][3].

in vivo

Linerixibat (GSK2330672; 0.05-10 mg/kg; oral gavage; twice daily; for 14 days; male ZDF rat) treatment lowers glucose in an animal model of type 2 diabetes^[1].

Animal Model:	Male Zucker Diabetic Fatty (ZDF) rat^[1]
Dosage:	0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg
Administration:	Oral gavage; twice daily; for 14 days
Result:	Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin.

References

[1] Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114. DOI:10.1021/jm400459m
[2] Wang Y, et al. HNF4α Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. Gene Expr. 2018 Aug 22;18(3):187-196. DOI:10.3727/105221618X15277685544442
[3] Linerixibat (GSK2330672) granted Orphan Status. September 24, 2019.

GSK 2330672 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK 2330672 Suppliers

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1345982-69-5, GSK 2330672Related Search:

GSK2814338 GSK-2256098 GSK-25 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine GSK 2801 GSK2636771 GSK2879552 GSK2795039 GSK2838232

GSK 2330672; GSK-2330672

GSK 2330672

3-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1λ<sup>6</sup>,4-benzothiazepin-8-yl]methylamino]pentanedioic acid

Pentanedioic acid, 3-((((3R,5R)-3-butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl)methyl)amino)-

CS-2639

Iinerixibat

linerixibat

Iinerixibat (GSK2330672)

type-2,PBC,lipid-lowering,solubility,nonabsorbable,GSK-2330672,Inhibitor,Primary,diabetes,GSK 2330672,Cholangitis,inhibit,Linerixibat,aqueous,Biliary,ASBT

linerixibat (GSK2330672)

3-((((3R,5R)-3-Butyl-3-ethyl-7-methoxy-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepin-8-yl)methyl)amino)pentanedioic acid

Linerixibat, 10 mM in DMSO

1345982-69-5