ChemicalBook > CAS DataBase List > GFB-8438

GFB-8438

Product Name
GFB-8438
CAS No.
2304549-73-1
Chemical Name
GFB-8438
Synonyms
GFB-8438;GFB-8438 ，S0750;GFB-8438, 10 mM in DMSO;4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one;4-Chloro-5-[3-oxo-4-(2-trifluoromethyl-benzyl)-piperazin-1-yl]-2H-pyridazin-3-one;3(2H)-Pyridazinone, 4-chloro-5-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]-1-piperazinyl]-;mouse,selective,Transient receptor potential channels,Inhibitor,inhibit,remodeling,TRP Channel,deoxycorticosterone,GFB 8438,loss,subtype,cytoskeletal,synaptopodin,podocytes,GFB8438,kidney,disease,acetate,GFB-8438
CBNumber
CB25855430
Molecular Formula
C16H14ClF3N4O2
Formula Weight
386.76
MOL File
2304549-73-1.mol
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GFB-8438 Property

Density 
1.52±0.1 g/cm3(Predicted)
solubility 
DMSO: Sparingly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml
form 
Solid
pka
9.09±0.60(Predicted)
color 
Off-white to light yellow
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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.

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

ChemScene
Product number
CS-0109395
Product name
GFB-8438
Purity
98.07%
Packaging
5mg
Price
$280
Updated
2021/12/16
ChemScene
Product number
CS-0109395
Product name
GFB-8438
Purity
98.07%
Packaging
10mg
Price
$480
Updated
2021/12/16
ChemScene
Product number
CS-0109395
Product name
GFB-8438
Purity
98.07%
Packaging
50mg
Price
$1400
Updated
2021/12/16
ChemScene
Product number
CS-0109395
Product name
GFB-8438
Purity
98.07%
Packaging
100mg
Price
$2250
Updated
2021/12/16
DC Chemicals
Product number
012754
Product name
GFB-8438
Packaging
001
Price
$650
Updated
2021/12/16
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GFB-8438 Chemical Properties,Usage,Production

Uses

GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model[1].

in vivo

GFB-8438 (30 mg/kg; s.c.; daily for 3 weeks) is efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of focal segmental glomerulosclerosis (FSGS), significantly reducing both total protein and albumin concentrations in urine[1].
GFB-8438 (1 mg/kg; i.v.) treatment shows the?Cl,?VSS,?and ?t1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively[1].

Animal Model:Sprague Dawley rats (DOCA-salt rat model of FSGS)[1]
Dosage:30 mg/kg
Administration:s.c.; daily for 3 weeks
Result:Significant reduction in urine protein concentrations.
Animal Model:6-8 weeks old male SD rats[1]
Dosage:1 mg/kg
Administration:i.v. (Pharmacokinetic?Analysis)
Result:The?Cl,?Vss,??and t1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively.

IC 50

hTRPC5: 0.18 μM (IC50); hTRPC4: 0.29 μM (IC50); rTRPC5: 0.18 μM (IC50)

References

[1] Yu M, et al.Discovery?of a?Potent?and?Selective?TRPC5?Inhibitor,?Efficacious?in a?Focal?Segmental?Glomerulosclerosis?Model.ACS Med Chem Lett.?2019 Oct 22;10(11):1579-1585. DOI:10.1021/acsmedchemlett.9b00430

GFB-8438 Preparation Products And Raw materials

Raw materials

Preparation Products

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GFB-8438 Suppliers

China 30 United States 4 Global 34
Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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021-65675885 18964387627
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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3008007409@qq.com
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Tianjin Kailiqi Biotechnology Co., Ltd.
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15076683720
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022-23754520
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Taizhou Crene Biotechnology Co. Ltd.
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+86-0576-88813233 +86-13396860566
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sales@pharm-intermediates.com
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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sales@chemegen.com
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CONIER CHEM AND PHARMA LIMITED
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InvivoChem
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2304549-73-1, GFB-8438 Related Search:


  • GFB-8438
  • 3(2H)-Pyridazinone, 4-chloro-5-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]-1-piperazinyl]-
  • 4-Chloro-5-[3-oxo-4-(2-trifluoromethyl-benzyl)-piperazin-1-yl]-2H-pyridazin-3-one
  • 4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one
  • mouse,selective,Transient receptor potential channels,Inhibitor,inhibit,remodeling,TRP Channel,deoxycorticosterone,GFB 8438,loss,subtype,cytoskeletal,synaptopodin,podocytes,GFB8438,kidney,disease,acetate,GFB-8438
  • GFB-8438, 10 mM in DMSO
  • GFB-8438 ，S0750
  • 2304549-73-1