| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
GPR40[1]
SCO-267 targets GPR40/FFAR1, a G protein-coupled receptor that is activated by free fatty acids. It acts as an allosteric full agonist. In CHO cells, SCO-267 activates Gαq, Gαs, and Gα12/13 pathways and induces β-arrestin recruitment. It shows allosteric modulation with fasiglifam and endogenous ligands. GPR40 activation stimulates insulin and incretin secretion. |
|---|---|
| ln Vitro |
The Gαq, Gαs, and Gα12/13 pathways, as well as β-Arrestin Recruitment, are activated by SCO-267 (CHO cells). With fasiglifam and an endogenous ligand, SCO-267 exhibits allosteric behavior[1].
In vitro, SCO-267 activates G protein-coupled receptor signaling pathways in CHO cells, including Gαq, Gαs, Gα12/13, and β-arrestin recruitment. It shows allosteric modulation with fasiglifam and endogenous ligands. The compound has an EC50 of 12 nM for GPR40/FFAR1 activation. |
| ln Vivo |
SCO-267 has a prolonged effect on reducing blood sugar levels and enhances insulin sensitivity (1 or 10 mg/kg; po)[1].
In vivo, SCO-267 (1 or 10 mg/kg; oral) improves insulin sensitivity and produces a prolonged effect on reducing blood sugar levels in N-STZ diabetic rat models. The compound effectively stimulates insulin secretion and GLP-1 release in diabetic rats, improving glucose tolerance. SCO-267 can be used for the research of type 2 diabetes. |
| Enzyme Assay |
The in vitro receptor activation assay for SCO-267 involves measuring GPR40-mediated signaling in CHO cells expressing the receptor. Calcium mobilization assays (Gαq pathway) or cAMP accumulation assays (Gαs pathway) are performed. β-arrestin recruitment is measured using BRET or ELISA-based assays. The EC50 value (12 nM) is determined from dose-response curves.
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| Cell Assay |
Cellular assays are performed using CHO cells expressing GPR40. Cells are treated with SCO-267 at varying concentrations. Receptor activation is assessed by measuring calcium flux, cAMP levels, or β-arrestin recruitment. Allosteric modulation is assessed by testing combinations with fasiglifam or endogenous ligands.
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| Animal Protocol |
Animal/Disease Models: N-STZ rats[1]
Doses: 1 or 10 mg/kg Route of Administration: Po; Experimental Results: Improved insulin sensitivity and exerted sustained glucose-lowering effect. In vivo animal studies are conducted in N-STZ (neonatal streptozotocin-induced) diabetic rat models. SCO-267 is administered orally at 1 or 10 mg/kg. Blood glucose levels are measured over time. Insulin sensitivity and GLP-1 secretion are assessed. |
| ADME/Pharmacokinetics |
SCO-267 is an orally active compound. It is soluble in DMSO at 80 mg/mL (130.13 mM). For in vivo administration, formulations can be prepared using 10% DMSO with 90% corn oil (3.3 mg/mL, 5.37 mM). Powder formulations should be stored at -20°C for up to 3 years; solutions should be stored at -80°C for up to 1 year.
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| Toxicity/Toxicokinetics |
Toxicity data for SCO-267 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized. The compound has been evaluated in preclinical studies in diabetic rat models.
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| References | |
| Additional Infomation |
GPR40 Full Agonist
SCO-267 is a research compound being investigated for the treatment of type 2 diabetes. It is a full agonist of GPR40/FFAR1 with an EC50 of 12 nM. The compound is available from commercial suppliers for research use only. It may be utilized in the study of chronic diseases including diabetes. |
| Molecular Formula |
C36H46N4O5
|
|---|---|
| Molecular Weight |
614.77
|
| Exact Mass |
614.346
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| CAS # |
1656261-09-4
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| PubChem CID |
90479828
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
6.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
45
|
| Complexity |
962
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(C1C=CC(OC)=CC=1N1CCC(COC2N=CC=C([C@H](C3CC3)CC(=O)O)C=2)CC1)(=O)N(C1=CC=CC(C)=N1)CC(C)(C)C
|
| InChi Key |
VVRXREQIOCYUKN-PMERELPUSA-N
|
| InChi Code |
InChI=1S/C36H46N4O5/c1-24-7-6-8-32(38-24)40(23-36(2,3)4)35(43)29-12-11-28(44-5)20-31(29)39-17-14-25(15-18-39)22-45-33-19-27(13-16-37-33)30(21-34(41)42)26-9-10-26/h6-8,11-13,16,19-20,25-26,30H,9-10,14-15,17-18,21-23H2,1-5H3,(H,41,42)/t30-/m0/s1
|
| Chemical Name |
(S)-3-Cyclopropyl-3-(2-((1-(5-methoxy-2-((6-methylpyridin-2-yl)(neopentyl)carbamoyl)phenyl)piperidin-4-yl)methoxy)pyridin-4-yl)propanoic acid
|
| Synonyms |
SCO267 SCO 267 SCO-267
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
DMSO : ~100 mg/mL (~162.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6266 mL | 8.1331 mL | 16.2662 mL | |
| 5 mM | 0.3253 mL | 1.6266 mL | 3.2532 mL | |
| 10 mM | 0.1627 mL | 0.8133 mL | 1.6266 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.
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