Synonym
PF-06291874; PF 06291874; PF06291874; PF-6291874; PF 6291874; PF6291874.
IUPAC/Chemical Name
(S)-3-(4-(1-(3,5-dimethyl-4-(4-(trifluoromethyl)-1H-pyrazol-1-yl)phenoxy)butyl)benzamido)propanoic acid
InChi Key
IBDYYOQKQCCSDP-QFIPXVFZSA-N
InChi Code
InChI=1S/C26H28F3N3O4/c1-4-5-22(18-6-8-19(9-7-18)25(35)30-11-10-23(33)34)36-21-12-16(2)24(17(3)13-21)32-15-20(14-31-32)26(27,28)29/h6-9,12-15,22H,4-5,10-11H2,1-3H3,(H,30,35)(H,33,34)/t22-/m0/s1
SMILES Code
O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C(C)=C2)N3C=C(C=N3)C(F)(F)F)CCC)C=C1)=O
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
>2 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
2934.99.9001
Biological target:
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist.
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
50.0 |
99.30 |
|
| DMSO |
75.0 |
148.95 |
|
| DMSO:PBS (pH 7.2) (1:1) |
0.5 |
0.99 |
|
| Ethanol |
0.5 |
0.99 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
503.52
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.
| 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 |
1: Wang M, Fu X, Du L, Shi F, Huang Z, Yang L. The Inferential Binding Sites of GCGR for Small Molecules Using Protein Dynamic Conformations and Crystal Structures. Int J Mol Sci. 2024 Aug 1;25(15):8389. doi: 10.3390/ijms25158389. PMID: 39125959; PMCID: PMC11313378.
2: Kazierad DJ, Chidsey K, Somayaji VR, Bergman AJ, Calle RA. Efficacy and safety of the glucagon receptor antagonist PF-06291874: A 12-week, randomized, dose-response study in patients with type 2 diabetes mellitus on background metformin therapy. Diabetes Obes Metab. 2018 Nov;20(11):2608-2616. doi: 10.1111/dom.13440. Epub 2018 Jul 30. PMID: 29923286.
3: Bergman A, Tan B, Somayaji VR, Calle RA, Kazierad DJ. A 4-week study assessing the pharmacokinetics, pharmacodynamics, safety, and tolerability of the glucagon receptor antagonist PF-06291874 administered as monotherapy in subjects with type 2 diabetes mellitus. Diabetes Res Clin Pract. 2017 Apr;126:95-104. doi: 10.1016/j.diabres.2017.01.019. Epub 2017 Feb 3. PMID: 28237861.
4: Kazierad DJ, Bergman A, Tan B, Erion DM, Somayaji V, Lee DS, Rolph T. Effects of multiple ascending doses of the glucagon receptor antagonist PF-06291874 in patients with type 2 diabetes mellitus. Diabetes Obes Metab. 2016 Aug;18(8):795-802. doi: 10.1111/dom.12672. Epub 2016 May 12. PMID: 27059951.
