Introduction：Basic information about Antide CAS 112568-12-4, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Antide Basic informationDescription
| Product Name: | Antide |
| Synonyms: | iturelix;Ac-D-2-Nal-4-chloro-D-Phe-beta-(3-pyridyl)-D-Ala-Ser-Lys(nicotinoyl)-D-Lys(nicotinoyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2;AC-DNAL-D: P-CLPHE-DPAL-SER-LYS: NICOTINOYL-DLYS: NICOTINOYL-LEU-LYS: ISOPROPYL-PRO-DALA-NH2;Brn 4866881;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N(sup 6)-(3-pyridinylcarbonyl)-L-lysyl-N(sup 6)-(3-pyridinylcarbonyl)-D-lysyl-L-leucyl-N(sup 6)-(1-methylethyl)-L-lysyl-L-prolyl-;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N6-(3-pyridinylcarbonyl)-L-lysyl-N6-(3-pyridinylcarbonyl)-D-lysyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-;Orf 23541;Ac-D-2-Nal-4-chloro-D-Phe-b-(3-pyridyl)-D-Ala-Ser-Lys(nicotinoyl)-D-Lys(nicotinoyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH2 |
| CAS: | 112568-12-4 |
| MF: | C82H108ClN17O14 |
| MW: | 1591.29 |
| EINECS: | |
| Product Categories: | hormones;Peptide;LH-RH;LH-RHPeptides for Cell Biology;Neuropeptides;Releasing Factors |
| Mol File: | 112568-12-4.mol |
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Antide Chemical Properties
| Boiling point | 1798.0±65.0 °C(Predicted) |
| density | 1.258±0.06 g/cm3(Predicted) |
| storage temp. | −20°C |
| pka | 12.78±0.46(Predicted) |
| form | Solid |
| color | White to off-white |
| InChIKey | QRYFGTULTGLGHU-NBERXCRTSA-N |
Safety Information
| Hazard Codes | T |
| Risk Statements | 60 |
| Safety Statements | 53-22-36/37/39-45 |
| WGK Germany | 3 |
| RTECS | AY2961700 |
| HS Code | 3504009000 |
Antide Usage And Synthesis
| Uses | Reversible inhibition of gonadotropin secretion and subsequent suppression of ovarian and testicular steroid secretio (gonadotropin releasing hormone antagonist). |
| Uses | Antide, is a GnRH and LH-RH antagonist, and with high anti-ovulatory and negligible histamine release activity. |
| Synthesis | Antide acetate was prepared as follows: the peptide intermediate was first treated with a suitable thiol to remove the Nps protecting group. It was then reacted with 2-benzyl-4-carboxypyridine in DMF in DCC as a coupling agent to acylate the Orn residue at the 5-position. After washing, the peptide resin was treated with piperidine to remove the Fmoc protecting group, followed by treatment with nicotinic acid and DIIC to acylate the D-Lys residue at the 6-position. Following cleavage and HPLC purification, the GnRH antagonist was tested and the peptide was considered effective in preventing ovulation in low-dose female mammals. |
| in vivo | Antide (subcutaneously; 1, 3, 6, 10 and 15 mg/kg; once or on 5 consecutive days) can induce a long-term chemical castration in adult male rats and cynomolgus monkeys[1]. | Animal Model: | Cynomolgus monkey and rat[1] | | Dosage: | 1, 3, 6, 10 and 15 mg/kg | | Administration: | Subcutaneous, once or on 5 consecutive days | | Result: | Had a dose-dependent inhibitory effect on serum concentration of LH (only rat) and testosterone and on the weights of the testes, prostates and seminal vesicles.
Achieved long-lasting castration-like effects at concentrations between 6 (less than or equal to 8 weeks) and 15 mg/kg (greater than 8 weeks) in the rat.
Induced a prolonged inhibitory effect only at 15 mg/kg and the duration was only 2-3 weeks in the cynomolgus monkey. |
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| Description | Antide acetate (Ac-AA10-NH2) is an LHRH antagonist and represses LH and FSH release from the pituitary gland. Antide Mw is 1590.6 Dalton. |
Antide Preparation Products And Raw materials
| Raw materials | BOC-D-4-Chlorophe-->(R)-N-Boc-(3-Pyridyl)alanine-->Boc-3-(2-Naphthyl)-D-alanine |
