GSK3039294 | CAS#1819986-22-5 | SAP inhibitor

MedKoo Cat#: 555377 | Name: GSK3039294

Description:

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

GSK3039294 is an orally available small molecule inhibitor of serum amyloid P component (SAP) binding to amyloid fibrils for the depletion of serum amyloid-P (SAP) component from the circulation.

Chemical Structure

GSK3039294

CAS#1819986-22-5

Theoretical Analysis

MedKoo Cat#: 555377

Name: GSK3039294

CAS#: 1819986-22-5

Chemical Formula: C30H44N2O14

Exact Mass: 656.2793

Molecular Weight: 656.68

Elemental Analysis: C, 54.87; H, 6.75; N, 4.27; O, 34.11

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Related CAS #

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Synonym

GSK3039294; GSK-3039294; GSK 3039294; amyloid P-IN-1; GSK294; GSK 294; GSK-294

IUPAC/Chemical Name

bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) adipoyl(R)-di-D-prolinate

InChi Key

KSKLDMGKWDUQCT-DNQXCXABSA-N

InChi Code

InChI=1S/C30H44N2O14/c33-25(31-13-3-5-23(31)27(35)41-19-43-29(37)45-21-9-15-39-16-10-21)7-1-2-8-26(34)32-14-4-6-24(32)28(36)42-20-44-30(38)46-22-11-17-40-18-12-22/h21-24H,1-20H2/t23-,24-/m1/s1

SMILES Code

O=C(N1[C@H](CCC1)C(OCOC(OC2CCOCC2)=O)=O)CCCCC(N3[C@H](CCC3)C(OCOC(OC4CCOCC4)=O)=O)=O

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:

amyloid P-IN-1 is used in the research of diseases or disorders wherein depletion of serum amyloid P component (SAP), including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.

In vitro activity:

GSK294 was highly soluble and stable in simulated gastric and intestinal fluids, stable in intestinal microsomes, and permeable in Madine Darby Canine Kidney type II cells. GSK294 was rapidly hydrolysed to miridesap and its mono pro-drug ester in blood and liver microsomes. Reference: Br J Pharmacol. 2020 Apr;177(8):1853-1864. https://pubmed.ncbi.nlm.nih.gov/31877231/

In vivo activity:

GSK294 showed good oral bioavailability of miridesap in rats and dogs. Reference: Br J Pharmacol. 2020 Apr;177(8):1853-1864. https://pubmed.ncbi.nlm.nih.gov/31877231/

	Solvent	mg/mL	mM
Solubility
	DMSO	34.0	51.78

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 656.68 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. Richards D, Bamford M, Liefaard L, Haque N, Lewis G, Storey J, Fernando D, Kumar S, Thompson D, Holmes DS. Identification, preclinical profile, and clinical proof of concept of an orally bioavailable pro-drug of miridesap. Br J Pharmacol. 2020 Apr;177(8):1853-1864. doi: 10.1111/bph.14956. Epub 2020 Feb 11. PMID: 31877231; PMCID: PMC7070169.

In vitro protocol:

In vivo protocol: