PF-04991532
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $1150 | Check With Us |
| 250mg | $1700 | Check With Us |
| 500mg | $2550 | Check With Us |
: Cat #: V4556 CAS #: 1215197-37-7 Purity ≥ 98%
Description: PF-04991532 is a novel, potent, hepatoselective glucokinase activator with EC50 of 80 and 100 nM in human and rat, respectively.
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| Molecular Weight (MW) | 396.36 |
|---|---|
| Molecular Formula | C18H19F3N4O3 |
| CAS No. | 1215197-37-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(O)C1=CN=C(NC([C@@H](N2C=C(C(F)(F)F)N=C2)CC3CCCC3)=O)C=C1 |
| Synonyms | PF-04991532; PF 04991532; PF04991532; PF-4991532; PF4991532; PF 4991532 |
| Protocol | In Vitro | PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 nM in human and 100 nM in rat and also a Phase 2 clinical candidate. Mechanistic experiments conducted in freshly isolated primary rat hepatocytes treated for 1 hour with PF-04991532 show increased 2-[14C]-deoxyglucose uptake (EC50 =1.261 µM) and increased glucose oxidation (EC50=5.769 µM). Additionally, PF-04991532 decreases the production of glucose from 1-[14C]-lactate in a dose dependent manner (EC50 =0.626 µM). In isolated rat hepatocytes, PF-04991532 increases the expression of G6Pase compare to cells treated only with 100 nM glucagon, and the greatest increase in G6Pase mRNA expression is in the presence of 25 mM glucose, 100 nM glucagon and PF-04991532. |
|---|---|---|
| In Vivo | A single dose of PF-04991532 increases the glucose infusion rate in order to maintain hyperglycemia. Despite the elevations in plasma triglycerides, surprisingly, hepatic triglycerides in rats dosed with 19 days of PF-04991532 are identical to vehicle treated GK rats. In an additional cohort treated for 28 days, identical hepatic lipid concentrations are observed between vehicle and rats dosed with PF-04991532 (Vehicle: 9.89±0.31; PF-04991532 100 mg/kg: 9.91±0.31). In rats treated with PF-04991532, there is increased expression of lipogenic gene expression such as acetyl-CoA carboxylase (ACC), ATP citrate lyase (ACLY), and fatty acid synthase (FAS). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.5230 mL | 12.6148 mL | 25.2296 mL | 50.4592 mL |
| 5mM | 0.5046 mL | 2.5230 mL | 5.0459 mL | 10.0918 mL |
| 10mM | 0.2523 mL | 1.2615 mL | 2.5230 mL | 5.0459 mL |
| 20mM | 0.1261 mL | 0.6307 mL | 1.2615 mL | 2.5230 mL |
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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