In Vivo
ChemicalBook > CAS DataBase List > PF06869206

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)
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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

Fujian boshi pharmaceutical technology co. LTD
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ShangHai Biochempartner Co.,Ltd
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17754423994 17754423994
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Shanghai Chaolan Chemical Technology Center
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QQ:65489617 15618227136
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Shanghai SuperLan Chemcial Technique Centre
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Zhejiang J&C Biological Technology Co.,Limited
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Career Henan Chemica Co
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laboratory@coreychem.com
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NINGBOBENKANGJS PHARMTECHCO., LTD
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DC Chemicals
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InvivoChem
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WEITIXIHAUGONG
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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:


  • 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