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Melanocortin (MC) Receptors(黑皮质素 (MC) 受体)

Melanocortin receptors (MCRs) comprise a family of five, class A, G protein-coupled receptors designated MC1R-MC5R with diverse physiological roles. MCRs are found in chordates and are regarded as having evolved from a single ancestral receptor, possibly corresponding most closely to MC4R. Signaling by MCRs has primarily been observed as occurring through the stimulatory α unit Gs which activates adenylyl cyclase to produce cAMP.

The central nervous melanocortin system is involved in energy homeostasis, regulating food intake and energy expenditure. The brain melanocortin system is defined as the primary neurons that express neuropeptide ligands, and secondary neurons expressing the predominant neural melanocortin receptors (MC3R, MC4R). Mutations in the gene encoding melanocortin receptor agonists, or the genes encoding MC3R or MC4R cause obesity. The other members of the melanocortin receptor family are primarily expressed in the periphery, and are involved in regulating pigmentation (MC1R), adrenal gland function (MC2R), immune function (MC1R/MC3R), and sebaceous gland activity (MC5R).

  1. Cat.No. 产品名称 Information
  2. GC66383 ACTH (11-24) (acetate)
  3. GC64525 Fenoprofen An NSAID
  4. GC64427 MK-0493
  5. GC63770 HS024 TFA
  6. GC63756 PG106 TFA
  7. GC63724 HS014 TFA
  8. GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide
  9. GC50303 MSG 606

    MSG-606 has potent antagonist activity and receptor selectivity for the human melanocortin 1 receptor (hMC1R) (IC50 = 17 nM) .

  10. GC38107 SNT-207858 free base
  11. GC38007 β-Melanocyte Stimulating Hormone (MSH), human TFA
  12. GC37629 Setmelanotide TFA
  13. GC36756 Nonapeptide-1 acetate salt An MC1R antagonist
  14. GC36727 Neuropeptide EI, rat
  15. GC35255 Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA
  16. GC35254 Adrenocorticotropic Hormone (ACTH) (1-39), rat
  17. GC35244 ACTH (1-17) TFA
  18. GC34231 γ-1-Melanocyte Stimulating Hormone (MSH), amide
  19. GC34002 Bremelanotide Acetate (PT-141 Acetate) A cyclic peptide agonist of MC4R
  20. GC33693 β-Melanocyte Stimulating Hormone (MSH), human (Beta-MSH (1-22) (human))
  21. GC32420 PF-00446687
  22. GC31954 ACTH 11-24 (Adrenocorticotropic Hormone (11-24))
  23. GC31629 MC-4R Agonist 1
  24. GC31600 SNT-207707
  25. GC31560 SNT-207858
  26. GC31109 ACTH 1-17 (α1-17-ACTH)
  27. GC30372 Setmelanotide (RM-493) Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.
  28. GC30194 JNJ-10229570 JNJ-10229570 (UNII-N9IX402L35) is a potent MC1R and MC5R antagonist.
  29. GC18458 Terrein A fungal metabolite with diverse biological activities
  30. GC13798 ML 00253764 hydrochloride A MC4R antagonist
  31. GC17626 PG 931 PG 931 是 SHU 9119 的类似物,是一种有效的黑皮质素 4 (MC4) 受体 (IC50\u003d0.58 nM) 激动剂,比对 hMC3R (IC50\u003d55 nM) 或 hMC5R (IC50\u003d2.4 nM) 更具选择性。
  32. GC12163 PG 106 PG 106 是一种有效的选择性人黑皮质素 3 (hMC3) 受体拮抗剂 (IC50\u003d210 nM),对 hMC4 受体 (EC50\u003d9900 nM) 和 hMC5 受体没有活性。
  33. GC13806 Lys-γ3-MSH Lys-γ3-MSH 是一种源自阿片黑皮质素原 (POMC) 片段 C 末端的黑皮质素肽。
  34. GC12239 ACTH (1-39) A MC2R agonist
  35. GC14127 MCL 0020 MCL 0020 是一种有效的选择性黑皮质素 MC4 受体拮抗剂,IC50 为 11.63 nM。
  36. GC10701 JKC 363 JKC 363 是一种选择性黑皮质素 MC4 受体拮抗剂,对 MC4 受体的亲和力 (IC50\u003d0.5 nM) 是对 MC3 受体 (44.9 nM) 的 90 倍。
  37. GC17002 γ1-MSH γ1-MSH 是一种黑皮质素 MC3 受体激动剂,对大鼠 MC3 受体的 Ki 值为 34 nM。
  38. GC13565 SHU 9119 An MC1R agonist and MC4R antagonist
  39. GC13068 [Nle4,D-Phe7]-α-MSH A synthetic analog of α-MSH
  40. GC10747 HS 024 HS 024 是一种选择性 MC4 受体拮抗剂,对 MC4、MC5、MC3 和 MC1 的 Kis 分别为 0.29、3.29、5.45 和 18.6 nM。
  41. GC12840 HS 014 HS 014 是一种有效的选择性黑皮质素 4 (MC4) 受体拮抗剂,对人 MC4、MC1、MC3 和 MC5 受体的 Kis 分别为 3.16、108、54.4 和 694 nM。
  42. GC10947 [D-Trp8]-γ-MSH An MC3R agonist
  43. GC16069 THIQ THIQ 是第一个选择性的黑皮质素 4 受体 (MC4R) 激动剂,对 hMC4R (IC50=1.2 nM, EC50=2.1 nM) 和 rMC4R (IC50=0.6 nM, EC50=2.9 nM) 具有高亲和力和效力。
  44. GC14374 α-MSH α-MSH (α-Melanocyte-Stimulating Hormone) 是一种内源性神经肽,是一种具有抗炎和解热活性的内源性黑皮质素受体 4 (MC4R) 激动剂。
  45. GC16276 Melanotan II A melanocortin receptor agonist

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