WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H555233
CAS#: 2227425-05-8
Description: 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).
Hodoodo Cat#: H555233
Name: PF-06869206
CAS#: 2227425-05-8
Chemical Formula: C15H14ClF3N4O2
Exact Mass: 374.08
Molecular Weight: 374.748
Elemental Analysis: C, 48.08; H, 3.77; Cl, 9.46; F, 15.21; N, 14.95; O, 8.54
Synonym: PF-06869206; PF 06869206; PF06869206;
IUPAC/Chemical Name: (S)-3-chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile
InChi Key: ATFQBBCQZKVZJN-QMMMGPOBSA-N
InChi Code: 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
SMILES Code: N#CC1=C(C(F)(F)F)N=C2C(NC(C)=C2Cl)=C1N3C[C@@H](CO)OCC3
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: Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solutecarrier (SLC) transporter located in the kidney proximal tubule that reabsorbs glomerularfiltered phosphate. Inhibition of NaPi2a may enhance urinary phosphate excretion and correct maladaptive mineral and hormonal derangements associated with increased cardiovascular risk in chronic kidney disease−mineral and bone disorder (CKD-MBD).
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The following data is based on the product molecular weight 374.75 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 |
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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
