PF-06869206
PF-06869206 is an Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1). PF-06869206 is the first orally bioavailable selective NaPi2a inhibitor and, as such, represents a pharmacological tool to probe the functional effects of selective NaPi2a inhibition in vivo. PF-06869206 showed a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). Furthermore, permeability is good (14 × 10−6 cm/s), and RLM clearance is low (<14 μL/min/mg; HLM = 39 μL/min/mg).
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Chemical Information
| Name | PF-06869206 |
|---|---|
| Iupac Chemical Name | (S)-3-chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile |
| Synonyms | PF-06869206; PF 06869206; PF06869206; |
| Molecular Formula | C15H14ClF3N4O2 |
| Molecular Weight | 374.7482 |
| Smile | N#CC1=C(C(F)(F)F)N=C2C(NC(C)=C2Cl)=C1N3C[C@@H](CO)OCC3 |
| InChiKey | ATFQBBCQZKVZJN-QMMMGPOBSA-N |
| InChi | InChI=1S/C15H14ClF3N4O2/c1-7-10(16)11-12(21-7)13(23-2-3-25-8(5-23)6-24)9(4-20)14(22-11)15(17,18)19/h8,21,24H,2-3,5-6H2,1H3/t8-/m0/s1 |
| CAS Number | 2227425-05-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | 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 |
| Handling | |
| 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1)
Kevin J. Filipski, Matthew F. Sammons, Samit K. Bhattacharya, Jane Panteleev, Janice A. Brown, Paula M. Loria, Markus Boehm, Aaron C. Smith, Andre Shavnya, Edward L. Conn, Kun Song, Yan Weng, Carie Facemire, Harald Jüppner, and Valerie Clerin
Publication Date (Web): April 12, 2018 (Letter)
DOI: 10.1021/acsmedchemlett.8b00013
Chemical Structure
