ChemicalBook > CAS DataBase List > PF 04995274

PF 04995274

Product Name
PF 04995274
CAS No.
1331782-27-4
Chemical Name
PF 04995274
Synonyms
PF 04995274;PF-04995274 ，S0496;PF04995274;PF 04995274;PF-04995274 >=98% (HPLC);PF-04995274, 10 mM in DMSO;4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol;(R)-4-((4-(((4-((Tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol;2H-Pyran-4-ol, tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-;Inhibitor,5-HT4,5-hydroxytryptamine Receptor,behavior,Alzheimer′s disease,PF-04995274,inhibit,PF04995274,Serotonin Receptor,5-HT Receptor,Stress-induced,PF 04995274,depressive-like
CBNumber
CB42668576
Molecular Formula
C23H32N2O6
Formula Weight
432.51
MOL File
1331782-27-4.mol
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PF 04995274 Property

storage temp. 
Store at -20°C
solubility 
DMSO:20.0(Max Conc. mg/mL);46.2(Max Conc. mM)
form 
A crystalline solid
color 
White to off-white
InChI
1S/C23H32N2O6/c26-23(7-12-27-13-8-23)16-25-9-4-17(5-10-25)14-29-22-21-19(30-18-6-11-28-15-18)2-1-3-20(21)31-24-22/h1-3,17-18,26H,4-16H2/t18-/m1/s1
InChIKey
WLLOFQROROXOMO-GOSISDBHSA-N
SMILES
OC1(CCOCC1)CN(CC2)CCC2COC3=NOC4=C3C(O[C@@H]5CCOC5)=CC=C4
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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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

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

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

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.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
28776
Product name
PF-04995274
Packaging
5mg
Price
$100
Updated
2024/03/01
Cayman Chemical
Product number
28776
Product name
PF-04995274
Packaging
25mg
Price
$412
Updated
2024/03/01
Cayman Chemical
Product number
28776
Product name
PF-04995274
Packaging
1mg
Price
$34
Updated
2024/03/01
Cayman Chemical
Product number
28776
Product name
PF-04995274
Packaging
10mg
Price
$183
Updated
2024/03/01
ChemScene
Product number
CS-0007316
Product name
PF-04995274
Purity
99.42%
Packaging
25mg
Price
$250
Updated
2021/12/16
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PF 04995274 Chemical Properties,Usage,Production

Description

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay). It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.

Uses

PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease[1][2][3].

in vivo

PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior[1].

Animal Model:Male 129S6/SvEv mice (7-8 weeks) treated with contextual fear conditioning (CFC) and forced swim test (FST)[1]
Dosage:3 mg/kg, 10 mg/kg
Administration:Intravenous injection; for 17 days
Result:Attenuated learned fear and decreased stress-induced depressive-like behavior.

IC 50

5-HT4 Receptor

References

[1] Chen BK, et al. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2019 Oct 10. DOI:10.1038/s41386-019-0540-3
[2] Grimwood S, et al. Translational receptor occupancy for the 5-HT4 partial agonist PF-04995274 in rats, non-human primates and healthy volunteers. Alzheimer’s Dement: J Alzheimer’s Assoc. 2011;7:S653.
[3] Timothy Nicholas1, et al. Systems pharmacology modeling in neuroscience: Prediction and outcome of PF-04995274, a 5-HT4 partial agonist, in a clinical scopolamine impairment trial. Advances in Alzheimer's Disease. Vol.2 No.3(2013).

PF 04995274 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 04995274 Suppliers

China 47 United States 3 USA 1 Global 51
Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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China
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Taizhou Tongxin Bio-Tech Co., Ltd
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0523-86818997 18652728585
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sales@allyrise.com
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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+86-21-52996696
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China
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4827
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Taizhou Ruixin Chemical Co., Ltd.
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0576-89085261 15867635987
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0576-89085262
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jasonhu09@163.com
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China
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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info@efebio.com
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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86249
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ShangHai Biochempartner Co.,Ltd
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177-54423994 17754423994
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QQ:2853530913
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2853530910@QQ.com
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China
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Beijing Solarbio Science & Tecnology Co., Ltd.
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010-50973130 18101056239
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3193328036@qq.com
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China
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Medi-tech Bioscientific Co., Ltd.
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0519-83246372 13585352506
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0519-83246372
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China
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Shanghai Biopharmaleader Co., Ltd.
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+86 18721201413
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+86 (21) 5775-8967
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sales@biopharmaleader.com
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1331782-27-4, PF 04995274Related Search:

PF 477736 PF-06700841-TsOH PF-06282999 PF 4618433 PF-06650833 PF-6260933 5-PyriMidinecarboxaMide, 4-[(2-Methylpropyl)aMino]-N-(phenylMethyl)-2-[4-[(tetrahydro-2H-pyran-3-yl)Methyl]-1-piperazinyl]- PF-01247324 PNU 100480 PF 05175157 PF 573228 PF-06882961 PF-5190457 PF-05212384 [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate PF-04691502 PF 3644022 Nirogacestat

  • PF 04995274
  • 4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol
  • PF04995274;PF 04995274
  • 2H-Pyran-4-ol, tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-
  • PF-04995274 >=98% (HPLC)
  • Inhibitor,5-HT4,5-hydroxytryptamine Receptor,behavior,Alzheimer′s disease,PF-04995274,inhibit,PF04995274,Serotonin Receptor,5-HT Receptor,Stress-induced,PF 04995274,depressive-like
  • (R)-4-((4-(((4-((Tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol
  • PF-04995274, 10 mM in DMSO
  • PF-04995274 ，S0496
  • 1331782-27-4