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MedKoo Cat#: 564933 | Name: PF-06372865

Description:

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

PF-06372865, also known as Darigabat, is a potent α2/3/5 subunit selective GABAa positive allosteric modulator.

Chemical Structure

PF-06372865
PF-06372865
CAS#1614245-70-3

Theoretical Analysis

MedKoo Cat#: 564933

Name: PF-06372865

CAS#: 1614245-70-3

Chemical Formula: C22H21FN4O3S

Exact Mass: 440.1318

Molecular Weight: 440.49

Elemental Analysis: C, 59.99; H, 4.81; F, 4.31; N, 12.72; O, 10.90; S, 7.28

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
PF06372865; PF 06372865; PF-06372865; Darigabat
IUPAC/Chemical Name
7-Ethyl-4-(4'-(ethylsulfonyl)-6-fluoro-2'-methoxybiphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine
InChi Key
PTTQXDBPTFOCMT-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H21FN4O3S/c1-4-27-13-24-21-18(12-25-26-22(21)27)14-6-9-19(23)17(10-14)16-8-7-15(11-20(16)30-3)31(28,29)5-2/h6-13H,4-5H2,1-3H3
SMILES Code
COC1=CC(S(=O)(CC)=O)=CC=C1C2=C(F)C=CC(C3=C4C(N(CC)C=N4)=NN=C3)=C2
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
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 440.49 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
1: Simen A, Whitlock M, Qiu R, Miceli J, Zumpano L, Du Metz M, Dua P, Binneman B. An 8-Week, Randomized, Phase 2, Double-Blind, Sequential Parallel-Group Comparison Study of Two Dose Levels of the GABAA Positive Allosteric Modulator PF-06372865 Compared With Placebo as an Adjunctive Treatment in Outpatients With Inadequate Response to Standard of Care for Generalized Anxiety Disorder. J Clin Psychopharmacol. 2019 Jan/Feb;39(1):20-27. doi: 10.1097/JCP.0000000000000997. PubMed PMID: 30531477. 2: Duveau V, Buhl DL, Evrard A, Ruggiero C, Mandé-Niedergang B, Roucard C, Gurrell R. Pronounced antiepileptic activity of the subtype-selective GABA(A) -positive allosteric modulator PF-06372865 in the GAERS absence epilepsy model. CNS Neurosci Ther. 2019 Feb;25(2):255-260. doi: 10.1111/cns.13046. Epub 2018 Aug 12. PubMed PMID: 30101518. 3: Gurrell R, Dua P, Feng G, Sudworth M, Whitlock M, Reynolds DS, Butt RP. A randomised, placebo-controlled clinical trial with the α2/3/5 subunit selective GABAA positive allosteric modulator PF-06372865 in patients with chronic low back pain. Pain. 2018 Sep;159(9):1742-1751. doi: 10.1097/j.pain.0000000000001267. PubMed PMID: 29787472. 4: Nickolls SA, Gurrell R, van Amerongen G, Kammonen J, Cao L, Brown AR, Stead C, Mead A, Watson C, Hsu C, Owen RM, Pike A, Fish RL, Chen L, Qiu R, Morris ED, Feng G, Whitlock M, Gorman D, van Gerven J, Reynolds DS, Dua P, Butt RP. Pharmacology in translation: the preclinical and early clinical profile of the novel α2/3 functionally selective GABA(A) receptor positive allosteric modulator PF-06372865. Br J Pharmacol. 2018 Feb;175(4):708-725. doi: 10.1111/bph.14119. Epub 2018 Jan 18. Erratum in: Br J Pharmacol. 2019 Jan;176(1):127. PubMed PMID: 29214652; PubMed Central PMCID: PMC5786456. 5: Zaccara G, Schmidt D. Antiepileptic Drugs in Clinical Development: Differentiate or Die? Curr Pharm Des. 2017;23(37):5593-5605. doi: 10.2174/1381612823666170809100524. PubMed PMID: 28799516.