Specification
Description
Sari 59-801 is a novel, orally effective hypoglycemic compound which appears to act largely, if not entirely, by stimulation of insulin release. The 2-hr hypoglycemic ED25 in fasting mice was 110 mg/kg; the plasma insulin levels were increased, with an ED50 of 47 mg/kg. Significant hypoglycemic activity was observed 2 hr after oral administration of 59-801 to fasting rats (ED25 = 86 mg/kg), while plasma insulin was elevated by 62% at 100 mg/kg. SARI-59-801 was more potent in producing hypoglycemia (ED25 = 47 mg/kg) than their lean littermates (ED25 = 131 mg/kg).
Synonyms
Sari 59-801; Sari-59-801; Sari59-801; Sari 59801; Sari-59801; Sari59801; Sandoz 59-801; Sandoz59-801; Sandoz-59-801
IUPAC Name
2-(dimethylamino)-1-(2-(3-ethyl-5-methylisoxazol-4-yl)-1H-indol-3-yl)ethan-1-ol
Canonical SMILES
OC(CN(C)C)C1=C(C2=C(C)ON=C2CC)NC3=C1C=CC=C3
InChI
InChI=1S/C18H23N3O2/c1-5-13-16(11(2)23-20-13)18-17(15(22)10-21(3)4)12-8-6-7-9-14(12)19-18/h6-9,15,19,22H,5,10H2,1-4H3
InChI Key
GMGOZCSXMVXXRS-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 68.98; H, 7.40; N, 13.41; O, 10.21
HS Tariff Code
2934.99.03.00
In Vitro Activity
59-801 stimulated insulin release by isolated rat islets at concentrations ranging from 0.05 to 0.3 mM.
Reference: Diabetes. 1985 Jun;34(6):548-52. https://pubmed.ncbi.nlm.nih.gov/3924691/
In Vivo Activity
SaRI 59-801 (Figure 1) has been found to be an effective oral hypoglycemic agent in normal mice, rats, and monkeys at doses ranging from 10 to 200 mg/kg.
Reference: Drug Development Research. 1985 6(1):67-77. https://onlinelibrary.wiley.com/doi/abs/10.1002/ddr.430060109
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).