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13

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T0293 Metyrapone

美替拉酮,甲吡酮,NSC-25265,Su-4885

Others; P450; Dehydrogenase; Autophagy Autophagy; Metabolism; Others
Metyrapone (NSC-25265) 是 STEROID 11-BETA-MONOOXYGENASE 酶抑制剂。 它被用作库欣综合征诊断中下丘脑-垂体反馈机制的测试。
T29112 VPC171

(2-氨基-4-(3-(三氟甲基)苯基)噻吩-3-基)(苯基)甲酮,VPC 171,VPC-171

Adenosine Receptor GPCR/G Protein; Neuroscience
VPC171 是一种新型腺苷 A1 受体正变构调节剂 (PAM)。
T0031L Ziprasidone hydrochloride

盐酸齐拉西酮,齐拉西酮盐酸盐,CP-88059 hydrochloride,CP-88059,Ziprasidone HCl

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Ziprasidone hydrochloride (CP-88059 hydrochloride) 是一种联合 5-HT(5-羟色胺)和多巴胺受体拮抗剂,具有抗精神病活性的强效作用。它也是去甲肾上腺素再摄取抑制剂。
T34383L 2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole, pregn-4-ene-3,20-dione deriv

Others Others
2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole, pregn-4-ene-3,20-dione deriv在Sprague Dawley大鼠上进行测试时显示出高局部抗炎效力和高肺选择性。
T34949 Trimethylolpropane caprate

UNII-X307CM75YF,Trimethylolpropane tridecanoate,Trimethylolpropane tricaprate

Trimethylolpropane caprate has developmental toxicity in Sprague-Dawley rats.
T37816 SB 243213

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1]. SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows...
T36949 Niaprazine

5-HT Receptor; Adrenergic Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。
T82886 Big endothelin-1 (rat 1-39)

Big endothelin-1 (rat 1-39) 是一个由39个氨基酸残基组成的多肽。它能在清醒状态的Sprague-Dawley大鼠中诱导利尿和利钠的反应,并可导致小鼠血压上升。
T61480 NHE3-IN-3

NHE3-IN-3 (Compound 1) is a potent inhibitor of the isoform 3 of the Na+/H+ exchanger (NHE3). It exhibits pIC50 values of 6.2 and 6.6 against human and rat NHE3, respectively. Furthermore, NHE3-IN-3 showcases exceptional oral bioavailability of 98% in SpragueDawley rats [1].
T64553 GLP-1(7-37) TFA salt

The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, ...
T71251 DS-1558

DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinog...
T37585 Ensartinib

Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N...
T37096 Sepimostat dimethanesulfonate

Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 μM[1]. Sepimostat (1 to 100 nmol/eye, intravitreal injection) exhibits significant neuroprotective effect[1]. ...

化合物

Metyrapone
Cat.No: T0293
Synonym: 美替拉酮,甲吡酮,NSC-25265,Su-4885
Target: Others, P450, Dehydrogenase, Autophagy
VPC171
Cat.No: T29112
Synonym: (2-氨基-4-(3-(三氟甲基)苯基)噻吩-3-基)(苯基)甲酮,VPC 171,VPC-171
Target: Adenosine Receptor
Ziprasidone hydrochloride
Cat.No: T0031L
Synonym: 盐酸齐拉西酮,齐拉西酮盐酸盐,CP-88059 hydrochloride,CP-88059,Ziprasidone HCl
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Norepinephrine, Histamine Receptor
2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole, pregn-4-ene-3,20-dione deriv
Cat.No: T34383L
Synonym:
Target: Others
Trimethylolpropane caprate
Cat.No: T34949
Synonym: UNII-X307CM75YF,Trimethylolpropane tridecanoate,Trimethylolpropane tricaprate
Target:
SB 243213
Cat.No: T37816
Synonym:
Target:
Niaprazine
Cat.No: T36949
Synonym:
Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor
Big endothelin-1 (rat 1-39)
Cat.No: T82886
Synonym:
Target:
NHE3-IN-3
Cat.No: T61480
Synonym:
Target:
GLP-1(7-37) TFA salt
Cat.No: T64553
Synonym:
Target:
DS-1558
Cat.No: T71251
Synonym:
Target:
Ensartinib
Cat.No: T37585
Synonym:
Target:
Sepimostat dimethanesulfonate
Cat.No: T37096
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1364 Ajugasterone C

筋骨草甾酮 C,筋骨草甾酮C

Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats.

天然产物

Ajugasterone C
Cat.No: TN1364
Synonym: 筋骨草甾酮 C,筋骨草甾酮C
Target:
TargetMol Loading
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