MedKoo Cat#: 530313 | Name: S-8510 free base

Description:

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

S-8510, also known as SB-737552, is a GABA-A receptor inverse agonist potentially for the treatment of dementia. S-8510 ameliorated memory impairment induced by cholinergic deficit in the water maze paradigm of Wistar rats. S-8510 augmented LTP of the Schaffer collateral/commissural fiber-CA1 synapses in the hippocampal slice preparations of SD rat. S-8510 increased the extracellular levels of acetylcholine and noradrenaline in the hippocampus of Wistar rat. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice.

Chemical Structure

S-8510 free base
S-8510 free base
CAS#151224-83-8 (free base)

Theoretical Analysis

MedKoo Cat#: 530313

Name: S-8510 free base

CAS#: 151224-83-8 (free base)

Chemical Formula: C12H10N4O2

Exact Mass: 242.0804

Molecular Weight: 242.24

Elemental Analysis: C, 59.50; H, 4.16; N, 23.13; O, 13.21

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
S-8510; SB-737552; S8510; SB737552; S 8510; SB 737552.
IUPAC/Chemical Name
2-(isoxazol-3-yl)-1,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine
InChi Key
ITPFSYAYHHPKRT-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H10N4O2/c1-3-17-6-7-8(1)13-5-10-11(7)15-12(14-10)9-2-4-18-16-9/h2,4-5H,1,3,6H2,(H,14,15)
SMILES Code
C12=NC=C3C(NC(C4=NOC=C4)=N3)=C1COCC2
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
>2 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
2934.99.9001
More Info
Related CAS# 151224-83-8 (S-8510 Free) 365279-39-6 (S-8510 phosphoric acid salt)

Preparing Stock Solutions

The following data is based on the product molecular weight 242.24 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
1: Chorvat RJ, Zaczek R, Brown BS. Ion channel modulators that enhance acetylcholine release: potential therapies for Alzheimer's disease. Expert Opin Investig Drugs. 1998 Apr;7(4):499-518. PubMed PMID: 15991988. 2: Kominami G, Nakamura M, Chomei N, Takada S. Radioimmunoassay for a novel benzodiazepine inverse agonist, S-8510, in human plasma and urine. J Pharm Biomed Anal. 1999 Jun;20(1-2):145-53. PubMed PMID: 10704018. 3: Tanaka H, Mizojiri K. Drug-protein binding and blood-brain barrier permeability. J Pharmacol Exp Ther. 1999 Mar;288(3):912-8. PubMed PMID: 10027826. 4: Abe K, Sawada T, Horiuchi M, Yoshimura K. Effects of S-8510, a benzodiazepine receptor partial inverse agonist, on event-related potentials (P300) in monkeys. Psychopharmacology (Berl). 1999 Jan;141(1):71-6. PubMed PMID: 9952067. 5: Abe K, Takeyama C, Yoshimura K. Effects of S-8510, a novel benzodiazepine receptor partial inverse agonist, on basal forebrain lesioning-induced dysfunction in rats. Eur J Pharmacol. 1998 Apr 24;347(2-3):145-52. PubMed PMID: 9653874. 6: Nezasa K, Higaki K, Takeuchi M, Yukawa T, Nakano M. Pharmacokinetics of a novel benzodiazepine partial inverse agonist in the F344 rat, SD rat and B6C3F1 mouse. Xenobiotica. 1998 May;28(5):515-25. PubMed PMID: 9622853. 7: Kawasaki K, Eigyo M, Ikeda M, Kihara T, Koike K, Matsushita A, Murata S, Shiomi T, Takada S, Yasui M. A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer. Prog Neuropsychopharmacol Biol Psychiatry. 1996 Nov;20(8):1413-25. PubMed PMID: 9004347. 8: Takada S, Sasatani T, Chomei N, Adachi M, Fujishita T, Eigyo M, Murata S, Kawasaki K, Matsushita A. Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51. PubMed PMID: 8709114.