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VU0453595

Product Name
VU0453595
CAS No.
1432436-13-9
Chemical Name
VU0453595
Synonyms
VU453595;VU0453595;VU0453595, 10 mM in DMSO;6-(2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)benzyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one;6-[[2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one;5H-Pyrrolo[3,4-b]pyridin-5-one, 6-[[2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6,7-dihydro-;Muscarinic acetylcholine receptor,modulator,systemically,allosteric,mAChR,PAM,positive,VU0453595,inhibit,schizophrenia,Inhibitor
CBNumber
CB04668659
Molecular Formula
C18H15FN4O
Formula Weight
322.34
MOL File
1432436-13-9.mol
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VU0453595 Property

Boiling point:
552.8±50.0 °C(Predicted)
Density 
1.35±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 100 mg/mL (310.23 mM; Need ultrasonic)
form 
Solid
pka
2.98±0.20(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

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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VU0453595 Chemical Properties,Usage,Production

Uses

VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140nM) for the research of schizophrenia[1][2].

Biological Activity

VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia[1][2]. Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs)[3]. VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD)[1].VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].

in vivo

VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD)[1].
VU0453595 (1-10mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].

Animal Model:Male C57BL6/J mice (8-9 weeks old)[1]
Dosage:1, 3, or 10mg/kg
Administration:Intraperitoneal (i.p.); 10mL/kg; administered 30min before the social interaction test
Result:Rescued deficits in social interaction observed in PCP-treated mice.

References

[1]. A Ghoshal, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610. [2]. Sean P Moran, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. [3]. Xiaohui Lv, et al. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222.

VU0453595 Preparation Products And Raw materials

Raw materials

Preparation Products

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VU0453595 Suppliers

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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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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Shanghai SuperLan Chemcial Technique Centre
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0-2022843681 15618226720
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+86-21-51601218
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chaolaichem@foxmail.com
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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InvivoChem
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+1-708-310-1919 +1-13798911105
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708-557-7486
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sales@invivochem.cn
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Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd
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15317229551
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QQ:3607245178
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15151849396@163.com
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China
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Bide Pharmatech Ltd.
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400-1647117 13681763483
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product02@bidepharm.com
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China
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TargetMol Chemicals Inc.
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4008200310
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marketing@tsbiochem.com
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China
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Shanghai Yifei Biotechnology Co. , Ltd.
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021-65675885 18964387627
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customer_service@efebio.com
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China
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Nanjing Shizhou Biology Technology Co.,Ltd
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025-85560043 15850508050
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025-85563444
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cindy.huang@synzest.com
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