醋酸特立帕肽
| 中文名稱(chēng) | 醋酸特立帕肽 |
|---|---|
| 中文同義詞 | 醋酸立特帕肽;特立帕肽;醋酸特立帕肽|PTH (1-34) (HUMAN);醋酸特立帕肽;重組人甲狀旁腺激素1-34;甲狀旁腺素(人);醋酸特立帕肽/重組人甲狀旁腺激素(1-34);醋酸特立帕肽 TERIPARATIDEACETATE |
| 英文名稱(chēng) | Teriparatide acetate |
| 英文同義詞 | PARATHYROID HORMONE HUMAN: FRAGMENT 1-34;PARATHYROID HORMONE (HUMAN, 1-34);PTH (HUMAN, 1-34);Teriparatide acetate;SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF;SER-VAL-SER-GLU-ILE-GLN-LEU-MET-HIS-ASN-LEU-GLY-LYS-HIS-LEU-ASN-SER-MET-GLU-ARG-VAL-GLU-TRP-LEU-ARG-LYS-LYS-LEU-GLN-ASP-VAL-HIS-ASN-PHE;SER-VAL-SER-GLU-ILE-GLN-LEU-MET-HIS-ASN-LEU-GLY-LYS-HIS-LEU-ASN-SER-MET-GLU-ARG-VAL-GLU-TRP-LEU-ARG-LYS-LYS-LEU-GLN-ASP-VAL-HIS-ASN-PHE HUMAN;Pth(1-34)(human) Acetate |
| CAS號(hào) | 52232-67-4 |
| 分子式 | C172H278N52O47S2 |
| 分子量 | 3890.49792 |
| EINECS號(hào) | 640-978-1 |
| 相關(guān)類(lèi)別 | 多肽中間體;醫(yī)藥原料藥;有機(jī)原料;蛋白質(zhì)/多肽;中間體;保護(hù)氨基酸;多肽;生物制藥;醫(yī)用原料;比例提取物;對(duì)照品;植物提取物;原料藥;標(biāo)準(zhǔn)產(chǎn)品;細(xì)胞生物學(xué)試劑;醫(yī)藥原料藥 科研原料;抑制劑;藥物多肽;多肽-藥物肽;標(biāo)準(zhǔn)品;定制多肽;肽類(lèi);僅供出口;日用化學(xué)品;比例提取物;原料藥;生物化工;化學(xué)產(chǎn)品;化學(xué)試劑;科研原料;Amino Acid Derivatives;Peptide;Hormones;Other Protein/Peptide Hormones;Parathyroid Hormone (PTH)Peptides and Proteins;Parathyroid Hormone Fragments;Peptides for Cell Biology;Peptides and Proteins;Various Peptides;EndocrinologyandHormones;proteins |
| Mol文件 | 52232-67-4.mol |
| 結(jié)構(gòu)式 | ![]() |
醋酸特立帕肽 性質(zhì)
| 熔點(diǎn) | >205oC (dec.) |
|---|---|
| RTECS號(hào) | SQ7770000 |
| 儲(chǔ)存條件 | −20°C |
| 溶解度 | DMSO(少許)、水(少許) |
| 形態(tài) | 粉末 |
| 顏色 | 白色至類(lèi)白色 |
| 生物來(lái)源 | human |
| 水溶解性 | Soluble to 0.40 mg/ml in water |
| 序列 | H-Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-Phe-OH |
| 穩(wěn)定性 | 吸濕性 |
| InChIKey | BUUKFBVDKSFMHN-LKMAISLMSA-N |
| CAS 數(shù)據(jù)庫(kù) | 52232-67-4(CAS DataBase Reference) |
特立帕肽皮下注射后吸收及消除速度都很快,皮下注射本品20 μg,達(dá)峰時(shí)間(tmax)為30 min,半衰期(t1/2 )為60 min,靜脈注射血清半衰期為5 min,絕對(duì)生物利用度95%。90%藥物經(jīng)腎臟清除。
醋酸特立帕肽常見(jiàn)不良反應(yīng)包括頭暈、背痛、惡心和下肢痙攣等,多為一過(guò)性;少見(jiàn)的不良反應(yīng)包括心律失常、耳聾等。目前認(rèn)為不良反應(yīng)發(fā)生與患者年齡和給藥劑量之間無(wú)明顯關(guān)系。
醋酸特立帕肽可通過(guò)抑制成骨細(xì)胞凋亡、激活骨襯細(xì)胞和增強(qiáng)成骨細(xì)胞分化來(lái)介導(dǎo)骨代謝。通過(guò)調(diào)節(jié)腺苷酸環(huán)化酶-環(huán)磷酸腺苷-蛋白激酶A傳導(dǎo)通路間歇性刺激成骨細(xì)胞、骨襯細(xì)胞和骨髓基質(zhì)干細(xì)胞表面PHT-Ⅰ受體,促進(jìn)成骨細(xì)胞的分化、延長(zhǎng)成骨細(xì)胞壽命;通過(guò)磷酸酯C-胞漿鈣離子-蛋白激酶C信號(hào)傳導(dǎo)通路,刺激成骨細(xì)胞系增殖;通過(guò)抑制PPARγ的反式激活活性,減少基質(zhì)細(xì)胞向脂肪細(xì)胞系分化,使成骨細(xì)胞數(shù)量增加;通過(guò)調(diào)節(jié)細(xì)胞因子間接調(diào)節(jié)骨的成長(zhǎng),例如可以誘導(dǎo)iGF-1與成骨細(xì)胞結(jié)合,從而促進(jìn)骨的形成;通過(guò)Wnt信號(hào)通路調(diào)節(jié)骨形成的過(guò)程,從而增加骨的形成。
禮來(lái)公司甲狀旁腺激素復(fù)泰奧(特立帕肽)最早批準(zhǔn)用于絕經(jīng)后婦女骨質(zhì)疏松 癥,初期或性腺機(jī)能減退的男性骨質(zhì)疏松癥患者,后來(lái)再次增加新適應(yīng)癥用于 在具有骨折高風(fēng)險(xiǎn)的治療與持久性、全身性糖皮質(zhì)激素治療有關(guān)的骨質(zhì)疏松。2011年復(fù)泰奧(特立帕肽)在全球銷(xiāo)售額達(dá)到9.51億美元。在中國(guó)市場(chǎng),2011 年由禮來(lái)(法國(guó))公司開(kāi)始進(jìn)口。Teriparatide (Human parathyroid hormone-(1-34)) 是 PHT 的激動(dòng)劑,其在 HEK293 細(xì)胞中的 IC50 值為 2 nM。
IC50: 2 nM (PTH).
Trabecular bone calcium and dry weight of the distal femur increased significantly in Teriparatide-treated animals. The increase in trabecular calcium compared with vehicle control occurred as early as 1 week after initiation of treatment with a 35% and 45% increase, respectively, for 10 μg/kg and 40 μg/kg Teriparatide. Similar results were observed for trabecular dry weight. After 4 weeks of treatment with 10 mg/kg or 40 mg/kg Teriparatide, trabecular calcium increased significantly by 70% and 123%, respectively, compared with the vehicle and by 73%.
The 4-week Teriparatide administration increase the pore ratio, number, and density as well as the cortical area, thickness, and bone mineral content (BMC), without significant influencing the volumetric bone mineral density (BMD). The 4-week Teriparatide administration + 8-week vehicle administration decrease the pore ratio, number, and density as well as the cortical area and thickness, compared with the 4-week Teriparatide administration, but the pore ratio, cortical area, and thickness are still higher compared with the 12-week vehicle administration. The 4-week Teriparatide administration + 8-week higherdose IBN administration increase the cortical area, thickness, BMC, and volumetric
BMD and decrease the pore ratio, but not the pore number or density, compared with the 4-week Teriparatide administration + 8-week vehicle administration.
單雜≤1.0%
醋酸根含量5.0%~12.0%
水分含量≤10.0%
肽含量≥80.0%
內(nèi)毒素≤5EU/mg
安全信息
| WGK Germany | 3 |
|---|---|
| 海關(guān)編碼 | 2937190000 |
| 存儲(chǔ)類(lèi)別 | 11 - 可燃固體 |
| 毒害物質(zhì)數(shù)據(jù) | 52232-67-4(Hazardous Substances Data) |
| 提供商 | 語(yǔ)言 |
|---|---|
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英文
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| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/07/06 | P1033 | Teriparatide Acetate | 52232-67-4 | 10mg | 1392.3元 |
| 2026/07/06 | P1033 | 醋酸特立帕肽 Teriparatide Acetate | 52232-67-4 | 50mg | 4176.9元 |
