| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
Sari 59-801 targets the pancreatic beta cells to stimulate insulin secretion, thereby lowering blood glucose levels. The compound appears to act largely by stimulation of insulin release. Additionally, Sari 59-801 has been reported to be a selective inhibitor of the protein kinase C (PKC) family, specifically targeting the PKCθ isoform. By inhibiting PKCθ, the compound may modulate immune responses, with potential applications in autoimmune diseases and transplant rejection.
|
|---|---|
| ln Vitro |
In vitro, Sari 59-801 stimulates insulin secretion from pancreatic beta cells, leading to increased plasma insulin levels. The compound's insulin secretagogue activity has been demonstrated in isolated islet or beta-cell preparations. As a PKCθ inhibitor, Sari 59-801 may also modulate immune cell function, although specific in vitro details are limited. The compound's hypoglycemic activity is mediated through its effects on insulin release rather than through direct insulin-mimetic effects.
|
| ln Vivo |
In vivo, Sari 59-801 has demonstrated potent hypoglycemic activity in several species. In fasted mice, the 2-hour hypoglycemic ED25 is 110 mg/kg, with a corresponding increase in plasma insulin levels (ED50 of 47 mg/kg). SARI-59-801 was more potent in producing hypoglycemia in obese mice (ED25 = 47 mg/kg) than in their lean littermates (ED25 = 131 mg/kg). In fasted rats, oral administration of Sari 59-801 produced significant hypoglycemic activity with an ED25 of 86 mg/kg after 2 hours, and a dose of 100 mg/kg increased plasma insulin levels by 62%.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Sari 59-801 are not extensively documented. However, as a PKCθ inhibitor, the compound's ability to inhibit PKCθ kinase activity can be assessed using kinase activity assays with recombinant PKCθ protein. The enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of Sari 59-801, and the extent of substrate phosphorylation is measured. The IC50 for inhibition of PKCθ activity is determined from dose-response curves.
|
| Cell Assay |
In vitro cellular assays for Sari 59-801 are performed using pancreatic beta-cell lines or primary islet cells to assess insulin secretion. Cells are treated with varying concentrations of Sari 59-801, and insulin levels in the culture supernatant are measured by ELISA or radioimmunoassay. For immune cell studies, T cells may be treated with Sari 59-801, and PKCθ-mediated signaling pathways such as NF-κB activation or cytokine production are assessed. Cell viability is evaluated using MTT assays to ensure that the observed effects are not due to cytotoxicity.
|
| Animal Protocol |
In vivo animal experiments for Sari 59-801 have been conducted in mouse and rat models. Fasted mice or rats are administered Sari 59-801 orally, and blood glucose levels are measured at various time points (e.g., 2 hours post-dose) to determine the hypoglycemic ED25. Plasma insulin levels are also measured to confirm the compound's insulin secretagogue activity. The compound's effects on body weight, food intake, and glucose tolerance may also be assessed in diabetic animal models.
|
| ADME/Pharmacokinetics |
Sari 59-801 has a molecular weight of 313.39 g/mol and a molecular formula of C18H23N3O2. The compound is soluble in DMSO at concentrations up to 65 mg/mL (207.41 mM). It is stable as a powder at -20°C for up to 3 years and in solution at -80°C for up to 1 year. The compound is orally active, supporting its use in in vivo studies. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported.
|
| Toxicity/Toxicokinetics |
Sari 59-801 has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. No significant toxicity has been reported in the available literature. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety profile for clinical development. As an insulin secretagogue, Sari 59-801 may have the potential to cause hypoglycemia at higher doses, which would need to be carefully managed.
|
| References | |
| Additional Infomation |
Sari 59-801 is a novel, orally effective hypoglycemic compound that acts largely by stimulating insulin release. It decreases blood glucose in several species and elevates plasma insulin in rats and mice. The compound is more potent in producing hypoglycemia in obese mice (ED25 = 47 mg/kg) than in lean littermates (ED25 = 131 mg/kg). Sari 59-801 is also a selective inhibitor of the PKCθ isoform with potential applications in autoimmune diseases and transplant rejection. It is a research compound and is not an approved drug.
|
| Molecular Formula |
C18H23N3O2
|
|---|---|
| Molecular Weight |
313.4
|
| Exact Mass |
313.179
|
| Elemental Analysis |
C, 68.98; H, 7.40; N, 13.41; O, 10.21
|
| CAS # |
80565-58-8
|
| PubChem CID |
133298
|
| Appearance |
Solid powder
|
| Density |
1.188g/cm3
|
| Boiling Point |
548.9ºC at 760 mmHg
|
| Flash Point |
285.8ºC
|
| Index of Refraction |
1.614
|
| LogP |
3.288
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
393
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCC1=NOC(=C1C2=C(C3=CC=CC=C3N2)C(CN(C)C)O)C
|
| 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
|
| Chemical Name |
2-(dimethylamino)-1-[2-(3-ethyl-5-methyl-1,2-oxazol-4-yl)-1H-indol-3-yl]ethanol
|
| Synonyms |
Sari-59-801 Sandoz 59-801 Sandoz59-801Sari 59-801Sari 59801 Sari-59801 Sari59801 Sandoz-59-801
|
| HS Tariff Code |
2934.99.03.00
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL | |
| 5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL | |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1908 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
