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.
MedKoo Cat#: 555377
Name: GSK3039294
CAS#: 1819986-22-5
Chemical Formula: C30H44N2O14
Exact Mass: 656.2793
Molecular Weight: 656.682
Elemental Analysis: C, 54.87; H, 6.75; N, 4.27; O, 34.11
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
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.0 | 51.78 |
The following data is based on the product molecular weight 656.682 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: | 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. |
