SML2306
CTEP
≥98% (HPLC)
別名:
2-Chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine, 2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine, RO4956371
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5 MG
￥24,800
25 MG
￥103,000
￥24,800
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品質そのまま、お求めになりやすい価格になりました。メルクは皆さんの科学発展を支えるパートナーとして製品を提供します。
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5 MG
￥24,800
25 MG
￥103,000
About This Item
￥24,800
Check Cart for Availability
品質そのまま、お求めになりやすい価格になりました。メルクは皆さんの科学発展を支えるパートナーとして製品を提供します。
バルクの問い合わせ
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アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
CC1=C(C#CC2=CC(Cl)=NC=C2)N=C(C)N1C3=CC=C(OC(F)(F)F)C=C3
InChI
1S/C19H13ClF3N3O/c1-12-17(8-3-14-9-10-24-18(20)11-14)25-13(2)26(12)15-4-6-16(7-5-15)27-19(21,22)23/h4-7,9-11H,1-2H3
InChI Key
GOHCTCOGYKAJLZ-UHFFFAOYSA-N
生物化学的／生理学的作用
Brain-penetrant, orally active, potent and selective mGluR5 (mGlu5) negative allosteric modulator & inverse agonist.
CTEP (RO4956371) may be used as a therapeutic to reduce hippocampal long-term depression, protein synthesis, and audiogenic seizures in the fragile X mental retardation 1 (Fmr1) knockout mouse.[1]
CTEP is a high-affinity, orally active, potent and selective metabotropic glutamate receptor 5 (mGlu5 or mGluR5) negative allosteric modulator (NAM) and inverse agonist (human/mouse/rat mGlu5 Kd = 1.7/1.8/1.5 nM; IC50 against quisqualate stimulation = 6.4/16.8/8/8 by IP accumulation or 11.4/42/4/6.9 by Ca2+ mobilization using human/mouse/rat mGlu5 HEK293 transfectants; IC50 = 40.1 nM against constitutive IP level in human mGlu5 HEK293) with >1000-fold selectivity over 103 molecular targets, including all known mGluRs. CTEP is an excellent tool compound for long-term in vivo studies (in mice and rats) with good pharmacokinetic properties (B/P ratio = 2.6, oral bioavailability ~100%, T1/2 ~18 hrs post 4.5 mg/kg p.o. in mice) and reported to display 30- to 100-fold higher in vivo potency than MPEP and fenobam in two rodent behavioral models sensitive to antianxiety drugs.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML2306-25MG:
SML2306-BULK:
SML2306-VAR:
SML2306-5MG:
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
Aubin Michalon et al.
Biological psychiatry, 75(3), 189-197 (2013-08-06)
Fragile X syndrome (FXS) is the most common genetic cause for intellectual disability. Fmr1 knockout (KO) mice are an established model of FXS. Chronic pharmacological inhibition of metabotropic glutamate receptor 5 (mGlu5) in these mice corrects multiple molecular, physiological, and
Stephanie A Barnes et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(45), 15073-15081 (2015-11-13)
Previous studies have hypothesized that diverse genetic causes of intellectual disability (ID) and autism spectrum disorders (ASDs) converge on common cellular pathways. Testing this hypothesis requires detailed phenotypic analyses of animal models with genetic mutations that accurately reflect those seen
Lothar Lindemann et al.
The Journal of pharmacology and experimental therapeutics, 339(2), 474-486 (2011-08-19)
The metabotropic glutamate receptor 5 (mGlu5) is a glutamate-activated class C G protein-coupled receptor widely expressed in the central nervous system and clinically investigated as a drug target for a range of indications, including depression, Parkinson's disease, and fragile X
Di Tian et al.
Nature neuroscience, 18(2), 182-184 (2015-01-13)
Human chromosome 16p11.2 microdeletion is the most common gene copy number variation in autism, but the synaptic pathophysiology caused by this mutation is largely unknown. Using a mouse with the same genetic deficiency, we found that metabotropic glutamate receptor 5
Aubin Michalon et al.
Neuron, 74(1), 49-56 (2012-04-17)
Fragile X syndrome (FXS) is the most common form of inherited intellectual disability. Previous studies have implicated mGlu5 in the pathogenesis of the disease, but a crucial unanswered question is whether pharmacological mGlu5 inhibition is able to reverse an already
アクティブなフィルタ
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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