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抑制剂&激动剂
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TargetMol产品目录中 "corticotropin-releasing factor receptor"的结果
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corticotropin-releasing factor receptor

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  • 抑制剂&激动剂
    34
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    2
    TargetMol | Recombinant_Protein
  • 多肽产品
    15
    TargetMol | Peptide_Products
  • 天然产物
    1
    TargetMol | Natural_Products
  • Urocortin, human
    Urocortin (human), Human urocortin I, Human urocortin 1, Human urocortin
    TP1021176591-49-4
    Urocortin, human (Human urocortin I) 是由 40 个氨基酸组成的神经多肽,是选择性 CRF2受体激动剂,作用于 hCRF1(Ki:0.4 nM)、rCRF2α(Ki:0.3 nM)、 mCRF2β(Ki:0.5 nM)。
    • ¥ 987
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • CP 376395
    CP-316311
    T4329175140-00-8
    CP 376395 (CP-316311)是一种 CRF1受体选择性拮抗剂。
    • ¥ 319
    In stock
    规格
    数量
  • Verucerfont
    NBI77860, 3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺, GSK561679
    T7361885220-61-1
    Verucerfont (NBI77860) 是促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂,作用于 CRF1(IC50:6.1 nM),CRF2 (IC50>1000 nM)和 CRF-BP (IC50>1000 nM)。
    • ¥ 538
    In stock
    规格
    数量
  • Crinecerfont
    SSR-125543A, SSR125543A, SSR-125543, SSR125543, SSR 125543A, SSR 125543
    T31095752253-39-7In house
    Crinecerfont (SSR-125543) 是促肾上腺皮质激素释放因子 1 受体 (CRF1) 的特异性拮抗剂,可用于经典先天性肾上腺增生的研究。
    • ¥ 774
    In stock
    规格
    数量
  • Pivagabine
    CXB-722, 匹伐加宾
    T1249269542-93-4
    Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物,具有神经调节活性。它可穿透大鼠的血脑屏障,拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。
    • ¥ 283
    In stock
    规格
    数量
  • NVS-CRF38
    T122761207258-55-6
    NVS-CRF38 is an antagonist of corticotropin-releasing factor receptor 1 (CRF1).
    • ¥ 11700
    6-8周
    规格
    数量
  • Emicerfont
    GW876008
    T15214786701-13-1
    Emicerfont is an antagonist of the corticotropin-releasing factor type 1 receptor (IC50: 66 nM).
    • ¥ 13900
    8-10周
    规格
    数量
  • Pexacerfont
    BMS-562086
    T16475459856-18-9
    Pexacerfont (BMS-562086) 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂,作用于人 CRF1 受体,IC50 为 6.1±0.6 nM。
    • ¥ 413
    In stock
    规格
    数量
  • NGD 98-2 hydrochloride
    T23067
    corticotropin-releasing factor receptor 1 (CRF1) antagonist
    • ¥ 5721
    待询
    规格
    数量
  • NGD9002
    NGD-9002,NGD 9002
    T25864666256-06-0
    NGD9002 is a novel generation, topology 2 selective corticotropin releasing factor-1 (CRF-1) receptor antagonist agent.
    • ¥ 12800
    8-10周
    规格
    数量
  • BMS-665053
    BMS665053
    T268551173435-64-7
    BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi
    • ¥ 10600
    6-8周
    规格
    数量
  • BMS-764459
    T268561188407-45-5
    BMS-764459 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1).
    • ¥ 15000
    8-10周
    规格
    数量
  • E2508
    E 2508,E-2508
    T27227685886-34-4
    E2508 is a selective antagonist of corticotropin-releasing factor 1 receptor.
    • ¥ 10600
    6-8周
    规格
    数量
  • Urocortin III (human) (trifluoroacetate salt)
    T35814
    Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).
    • ¥ 7043
    待询
    规格
    数量
  • r 121919 hydrochloride
    T38228195055-66-4
    High affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable. Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216 |Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID:15696320 |Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID:12538845 |Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID:12093593
    • 待估
    35日内发货
    规格
    数量
  • ONO-2333
    T69248441060-02-2
    ONO-2333 is a corticotropin-releasing factor receptor antagonist, for the treatment of depression and or anxiety disorders
    • ¥ 10600
    6-8周
    规格
    数量
  • NGD 98-2
    T69374355836-54-3
    NGD 98-2 is a new generation, topology 2 selective orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
    • ¥ 10600
    6-8周
    规格
    数量
  • Antalarmin
    T70433157284-96-3
    Antalarmin 是一种可通过血脑屏障具有选择性和高效性的促肾上腺皮质激素释放因子受体 1 (CRHR1) 拮抗剂,可阻断促肾上腺皮质激素释放激素诱导的大鼠高血压,阻断CRF激活,抑制卡拉胶素诱导的大鼠皮下炎症。
    • ¥ 10600
    1-2周
    规格
    数量
  • BMS-763534
    T712941188407-40-0
    BMS-763534 is a potent antagonist of corticotropin-releasing factor hormone receptor 1 (CRHR-1).
    • ¥ 13900
    8-10周
    规格
    数量
  • urocortin ii, mouse
    T76127330648-32-3
    Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂,对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP PKA 和 Ca2+ CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达,并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。
    • 待询
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    数量
  • Urocortin III (human)
    T76180357952-09-1
    Urocortin III (human) 是一种促肾上腺皮质激素释放因子 (CRF) 相关肽。Urocortin III (human) 优先结合并激活CRF-R2,并且具有离散的中枢神经系统和外周分布。Urocortin III (human) 选择性结合 2 型 CRF 受体,mCRF2β、rCRF2α 和 hCRF1 的Ki 值分别为 13.5、21.7 和 >100 nM。Urocortin III (human) 介导Insulin(human) 分泌的生长抑素依赖性负反馈控制。
    • 待估
    35日内发货
    规格
    数量
  • (Tyr0)-Urocortin, rat
    T76492187111-93-9
    (Tyr0)-Urocortin, rat 是针对促肾上腺皮质激素释放因子受体1型(CRF-R1)和2型(CRF-R2)的高亲和力激动剂,其抑制结合常数(Ki)为1-2 nM。
    • 待询
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    数量
  • K 41498 TFA
    T83674
    K 41498 是一种针对皮质酮释放因子受体2α(CRF2α)和CRF2β的肽拮抗剂,其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性,与CRF1相比(在表达人类受体的HEK293细胞中Ki值为425 nM)。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药,K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。
    • 待估
    规格
    数量
  • Urocortin II (human) TFA
    T85181398001-88-2
    Urocortin II, a neuropeptide hormone within the corticotropin-releasing factor (CRF) family—which comprises mammalian CRF, urocortin I, urocortin III, frog sauvagine, and piscine urotensin I—displays 34, 43, and 37-40% sequence homology with rat and human CRF, human urocortin I, and human urocortin III, respectively. This compound enhances rabbit ventricular myocyte shortening and relaxation in both a time- and concentration-dependent manner. In vivo studies reveal that urocortin II lowers arterial blood pressure in both normotensive and spontaneously hypertensive rats through peripheral CRF2 receptor agonism, inducing dose-dependent tachycardia and hypotension at doses of 3 and 30 pmol/kg. Additionally, it mitigates the visceral pain response to colorectal distension at 10 and 20 μg/kg in conscious rats and delays gastric emptying in mice.
    • 待询
    8-10周
    规格
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