MedKoo Cat#: 461814 | Name: SARI-59-801
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Description:

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

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).

Chemical Structure

SARI-59-801
SARI-59-801
CAS#80565-58-8

Theoretical Analysis

MedKoo Cat#: 461814

Name: SARI-59-801

CAS#: 80565-58-8

Chemical Formula: C18H23N3O2

Exact Mass: 313.1790

Molecular Weight: 313.40

Elemental Analysis: C, 68.98; H, 7.40; N, 13.41; O, 10.21

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to ship
5mg USD 350.00 Ready to ship
10mg USD 550.00 Ready to ship
25mg USD 950.00 Ready to ship
50mg USD 1,650.00 Ready to ship
100mg USD 2,850.00 Ready to ship
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Synonym
Sari 59-801; Sari-59-801; Sari59-801; Sari 59801; Sari-59801; Sari59801; Sandoz 59-801; Sandoz59-801; Sandoz-59-801;
IUPAC/Chemical Name
2-(dimethylamino)-1-(2-(3-ethyl-5-methylisoxazol-4-yl)-1H-indol-3-yl)ethan-1-ol
InChi Key
GMGOZCSXMVXXRS-UHFFFAOYSA-N
InChi Code
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
SMILES Code
OC(CN(C)C)C1=C(C2=C(C)ON=C2CC)NC3=C1C=CC=C3
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
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.
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

Preparing Stock Solutions

The following data is based on the product molecular weight 313.40 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. Hanson RL, Isaacson CM. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Relation to cAMP concentration and Ca2+ uptake. Diabetes. 1985 Jul;34(7):691-5. doi: 10.2337/diab.34.7.691. PMID: 2408949. 2. Hanson RL, Isaacson CM, Boyajy LD. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Diabetes. 1985 Jun;34(6):548-52. doi: 10.2337/diab.34.6.548. PMID: 3924691. 3. Ho RS, Wiseberg JJ, Brand LJ, Nadelson J, Boyajy LD. A novel, orally effective hypoglycemic agent, SaRI 59-801, in laboratory animals. Drug Development Research. 1985 6(1):67-77. doi: 10.1002/ddr.430060109.
In vitro protocol:
1. Hanson RL, Isaacson CM. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Relation to cAMP concentration and Ca2+ uptake. Diabetes. 1985 Jul;34(7):691-5. doi: 10.2337/diab.34.7.691. PMID: 2408949. 2. Hanson RL, Isaacson CM, Boyajy LD. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Diabetes. 1985 Jun;34(6):548-52. doi: 10.2337/diab.34.6.548. PMID: 3924691.
In vivo protocol:
1. Ho RS, Wiseberg JJ, Brand LJ, Nadelson J, Boyajy LD. A novel, orally effective hypoglycemic agent, SaRI 59-801, in laboratory animals. Drug Development Research. 1985 6(1):67-77. doi: 10.1002/ddr.430060109.
1: Hanson RL, Isaacson CM. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Relation to cAMP concentration and Ca2+ uptake. Diabetes. 1985 Jul;34(7):691-5. PubMed PMID: 2408949. 2: Hanson RL, Isaacson CM, Boyajy LD. Stimulation of insulin secretion from isolated rat islets by SaRI 59-801. Diabetes. 1985 Jun;34(6):548-52. PubMed PMID: 3924691. Tse FL, Orwig B, Jaffe JM. Disposition of alpha-[(dimethylamino)methyl]-2-(3-ethyl-5-methyl-4-isoxazolyl)- 1H-indole-3-methanol (59-801), a hypoglycaemic agent in rats, dogs and monkeys. Xenobiotica. 1987 Jun;17(6):741-9. doi: 10.3109/00498258709043981. PMID: 3630208.