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MedKoo Cat#: 463890 | Name: PF-06928215
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Description:

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

PF-06928215 is an inhibitor of cyclic GMP-AMP synthase.

Chemical Structure

PF-06928215
PF-06928215
CAS#2378173-15-8

Theoretical Analysis

MedKoo Cat#: 463890

Name: PF-06928215

CAS#: 2378173-15-8

Chemical Formula: C20H20N4O4

Exact Mass: 380.1485

Molecular Weight: 380.40

Elemental Analysis: C, 63.15; H, 5.30; N, 14.73; O, 16.82

Price and Availability

Size Price Availability Quantity
5mg USD 425.00 2 Weeks
25mg USD 900.00 2 Weeks
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Related CAS #
No Data
Synonym
PF-06928215; PF06928215; PF 06928215;
IUPAC/Chemical Name
(1R,2S)-2-(7-hydroxy-5-phenylpyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexane-1-carboxylic acid
InChi Key
PHGTYMRDHDEHLI-HIFRSBDPSA-N
InChi Code
InChI=1S/C20H20N4O4/c25-17-10-16(12-6-2-1-3-7-12)22-18-14(11-21-24(17)18)19(26)23-15-9-5-4-8-13(15)20(27)28/h1-3,6-7,10-11,13,15,25H,4-5,8-9H2,(H,23,26)(H,27,28)/t13-,15+/m1/s1
SMILES Code
OC([C@@H]1CCCC[C@@H]1NC(C2=C3N(C(O)=CC(C4=CC=CC=C4)=N3)N=C2)=O)=O
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
>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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ.
In vitro activity:
Notably, compound 19 and PF-06928215 have binding affinities of 2.7 and 0.2 μM, respectively, with a corresponding increase in inhibitory potency in the cGAS assay; PF-06928215 inhibited cGAS activity with an IC50 value of 4.9 μM (Fig 5A). As with other compounds, there is good agreement between binding and inhibition, though activity measurements occur in the presences of competing nucleotides which would cause the IC50 to appear weaker than KD measurements conducted without nucleotides. Compared to compound 15, PF-06928215 has improved in potency and displays longer off rate kinetics than any other compound in this series (Figs (Figs4C4C and and5B5B). Reference: PLoS One. 2017 Sep 21;12(9):e0184843. https://pubmed.ncbi.nlm.nih.gov/28934246/
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 31.7 83.24
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 380.40 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
Formulation protocol:
Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K. Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. PLoS One. 2017 Sep 21;12(9):e0184843. doi: 10.1371/journal.pone.0184843. PMID: 28934246; PMCID: PMC5608272.
In vitro protocol:
Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K. Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. PLoS One. 2017 Sep 21;12(9):e0184843. doi: 10.1371/journal.pone.0184843. PMID: 28934246; PMCID: PMC5608272.
In vivo protocol:
TBD
1: Gong Y, Li G, Tao J, Wu NN, Kandadi MR, Bi Y, Wang S, Pei Z, Ren J. Double knockout of Akt2 and AMPK accentuates high fat diet-induced cardiac anomalies through a cGAS-STING-mediated mechanism. Biochim Biophys Acta Mol Basis Dis. 2020 Oct 1;1866(10):165855. doi: 10.1016/j.bbadis.2020.165855. Epub 2020 Jun 5. PMID: 32512189. 2: Zhao W, Xiong M, Yuan X, Li M, Sun H, Xu Y. In Silico Screening-Based Discovery of Novel Inhibitors of Human Cyclic GMP-AMP Synthase: A Cross- Validation Study of Molecular Docking and Experimental Testing. J Chem Inf Model. 2020 Jun 22;60(6):3265-3276. doi: 10.1021/acs.jcim.0c00171. Epub 2020 Jun 9. PMID: 32459092. 3: Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K. Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. PLoS One. 2017 Sep 21;12(9):e0184843. doi: 10.1371/journal.pone.0184843. PMID: 28934246; PMCID: PMC5608272. Wang X, Lu W, Xia X, Zhu Y, Ge C, Guo X, Zhang N, Chen H, Xu S. Selenomethionine mitigate PM2.5-induced cellular senescence in the lung via attenuating inflammatory response mediated by cGAS/STING/NF-κB pathway. Ecotoxicol Environ Saf. 2022 Dec 1;247:114266. doi: 10.1016/j.ecoenv.2022.114266. Epub 2022 Nov 2. PMID: 36334339.