PF06869206

In Vivo

Product Name: PF06869206
CAS No.: 2227425-05-8
Chemical Name: PF06869206
Synonyms: CS-2762;PF06869206;PF-06869206;PF-06869206; PF 06869206; PF06869206;inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206;(S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile;1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)-
CBNumber: CB04187431
Molecular Formula: C15H14ClF3N4O2
Formula Weight: 374.75
MOL File: 2227425-05-8.mol

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PF06869206 Property

Boiling point:: 599.2±50.0 °C(Predicted)
Density: 1.57±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMF: 1 mg/mL; DMSO: 1mg/mL; Ethanol: 10mg/mL; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/mL
form: A crystalline solid
pka: 11.78±0.40(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 28158
Product name: PF-06869206
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 28158
Product name: PF-06869206
Packaging: 25mg
Price: $533
Updated: 2024/03/01

Cayman Chemical

Product number: 28158
Product name: PF-06869206
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 28158
Product name: PF-06869206
Packaging: 10mg
Price: $243
Updated: 2024/03/01

ChemScene

Product number: CS-0043242
Product name: PF-06869206
Purity: 99.85%
Packaging: 25mg
Price: $260
Updated: 2021/12/16

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PF06869206 Chemical Properties,Usage,Production

In Vivo

PF-06869206 is evaluated in rodent PK studies to determine suitability for in vivo pharmacology exploration. Results show moderate clearance in both rat and mouse. Oral bioavailability at 5 mg/kg is good in rat and moderate in mouse. At higher oral doses of 50 mg/kg, supraproportional increases in exposure are observed in both species, suggestive of saturation of clearance. PF-06869206 has moderate terminal elimination half-life (t1/2=1.35 h, and 0.75 h for Wistar-Han rats (10 mg/kg, iv), and C57BL6 mice (1 mg/kg, iv)). Furthermore, permeability is good (14×10-6 cm/s), and rat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM=39 μL/min/mg).

Description

PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC₅₀ = 380 nM). It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC₅₀s = >25 μM).

Biological Activity

PF-06869206 (PF06869206) is a potent, selective, orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a/SLC34A1) with IC50 of 380 nM, no inhibition against NaPi2b (SLC34A2) and NaPi2c (SLC34A3).PF-06869206 displays excellent subtype selectivity against other sodium-phosphate cotransporters: NaPi2b, NaPi2c, PiT-1, and PiT-2 (SLC20A2).PF-06869206 showed comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms (IC50=0.4-0.54 uM) and was selective over rodent NaPi2c, inhibited phosphate uptake in human proximal tubule cells.PF-06869206 was well tolerated and elicited a dose-dependent increase in fractional phosphate excretion, lowered plasma phosphate levels in WT mice and in rats with chronic kidney disease (CKD), induced an unabated acute phosphaturic and hypophosphatemic effect in CKD rats.

in vitro

PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines. PF-06869206 shows comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms with IC50s of 0.4±0.047 μM and 0.54±0.099 μM for rat NaPi2a and mouse NaPi2a, respectively.

PF06869206 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF06869206 Suppliers

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View Lastest Price from PF06869206 manufacturers

Career Henan Chemica Co

Product: PF06869206 2227425-05-8
Price: US $0.01/KG
Min. Order: 1KG
Purity: 95%-99%
Supply Ability: 1kg; 5kg; 10kg
Release date: 2020-10-28

2227425-05-8, PF06869206Related Search:

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PF06869206

PF-06869206

CS-2762

PF-06869206; PF 06869206; PF06869206

1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)-

(S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile

inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206

2227425-05-8