L2761

[des-Gly¹⁰, D-His(Bzl)⁶]-LH-RH ethylamide

≥97% (HPLC), powder

• 别名: Histrelin
• 经验公式（希尔记法）: C₆₆H₈₆N₁₈O₁₂
• CAS号: 76712-82-8
• 分子量: 1323.50
• MDL號碼: MFCD00133494
• 分類程式碼代碼: 12352209
• PubChem物質ID: 24896325
• NACRES: NA.32

属性

• 品質等級: 200
• 化驗: ≥97% (HPLC)
• 形狀: powder
• 成份: Peptide content, ~70%
• UniProt登錄號: P55248; P01148; P07490; P13562; P30968; P30969; Q01776
• 儲存溫度: −20°C
• SMILES 字串: CCNC(=O)C1CCCN1C(=O)C(CCCNC(N)=N)NC(=O)C(CC(C)C)NC(=O)C(Cc2cn(Cc3ccccc3)cn2)NC(=O)C(Cc4ccc(O)cc4)NC(=O)C(CO)NC(=O)C(Cc5c[nH]c6ccccc56)NC(=O)C(Cc7cnc[nH]7)NC(=O)C8CCC(=O)N8
• InChI: 1S/C66H86N18O12/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71)
• InChI 密鑰: HHXHVIJIIXKSOE-UHFFFAOYSA-N
• 基因資訊: human ... GNRH1(2796) , GNRHR(2798) ; mouse ... GNRH1(14714) , GNRHR(14715) ; rat ... GNRH1(25194) , GNRHR(81668)

说明

Amino Acid Sequence

Glp-His-Trp-Ser-Tyr-His(Bzl)-Leu-Arg-Pro-NHEt

應用

[des-Gly¹⁰, D-His(Bzl)⁶]-LH-RH ethylamide has been used:

• for inducing Batrachoseps gravid females to oviposit
• for comparing the effect of LHRH (luteinizing hormone-releasing hormone) agonists and dopamine antagonists in Lithobates pipiens
• for inducing oviposition in females of Taricha granulosa and Ensatina eschscoltzii
• to induce spawning in Spea hammondii adults

生化／生理作用

Glp-His-Trp-Ser-Tyr-His(Bzl)-Leu-Arg-Pro-NHEt ([des-Gly¹⁰, D-His(Bzl)⁶]-LH-RH) is a GnRH (gonadotropin-releasing hormone) agonist, histerelin. GnRH (Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), which is also referred as LHRH (luteinizing hormone-releasing hormone) or gonadorelin, is crucial for mammalian reproduction and is released from hypothalamic neurons. It is responsible for the secretion of gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), from the pituitary glands. Mutations in GnRH are associated with normosmic congenital hypogonadotropic hypogonadism. Histerelin is used for the treatment of central precocious puberty in children. It inhibits actions of sex steroids on the male and female reproductive organs.

特點和優勢

Has greater lipophilicity than other LH-RH agonists, but retains high water solubility

安全信息

• 象形圖: GHS08
• 訊號詞: Danger
• 危險聲明: H360
• 防範說明: P201 - P308 + P313
• 危險分類: Repr. 1B
• 儲存類別代碼: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable
• 個人防護裝備: Eyeshields, Gloves, type P3 (EN 143) respirator cartridges