GSK3039294
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555377

CAS#: 1819986-22-5

Description: 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

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GSK3039294
CAS# 1819986-22-5

Theoretical Analysis

MedKoo Cat#: 555377
Name: GSK3039294
CAS#: 1819986-22-5
Chemical Formula: C30H44N2O14
Exact Mass: 656.28
Molecular Weight: 656.682
Elemental Analysis: C, 54.87; H, 6.75; N, 4.27; O, 34.11

Price and Availability

Size Price Availability Quantity
50mg USD 450
100mg USD 750
200mg USD 1250
500mg USD 2150
1g USD 3150
2g USD 5850
5g USD 8650
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Synonym: GSK3039294; GSK-3039294; GSK 3039294;

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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.0 51.78

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.

Recalculate based on batch purity %
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: 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 vivo 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.

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