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52232-67-4

中文名稱 醋酸特立帕肽
英文名稱 Teriparatide acetate
CAS 52232-67-4
分子式 C181H291N55O51S2
MDL 編號 MFCD00149013
分子量 4117.72
MOL 文件 52232-67-4.mol
更新日期 2024/12/20 09:35:54
52232-67-4 結構式 52232-67-4 結構式

基本信息

中文別名
醋酸特立帕肽
醋酸立特帕肽
特立帕肽
立特帕肽(TERIPARATIDE)
英文別名
[CYS5,28] PARATHYROID HORMONE (1-34), HUMAN
[CYS5,28] PTH (1-34), HUMAN
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
PARATHYROID HORMONE (1-34), HUMAN
PARATHYROID HORMONE (HUMAN, 1-34)
PARATHYROID HORMONE HUMAN: FRAGMENT 1-34
PTH (1-34) (HUMAN)
PTH (HUMAN, 1-34)
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
SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF
TERIPARATIDE
Teriparatide acetate
Pth(1-34)(human) Acetate
PARATHYROID HORMONE FRAGMENT HUMAN 1-34 APPROX. 95%
PARATHYROID HORMONE FRAGMENT HUMAN 1-34 90-95%
Teriparatide, Parathyroid Hormone(1-34),human
parathyroid hormone fragment 1-34 human
PARATHYROID HORMONE (PTH) HUMAN 1-34, MIN 95%
(1-34)-HUMAN PARATHYROID HORMONE
所屬類別
生物化工:其他保護氨基酸

物理化學性質

熔點>205oC (dec.)
RTECS號SQ7770000
儲存條件−20°C
儲存條件−20°C
溶解度DMSO(少許)、水(少許)
形態(tài)powder
顏色白色至灰白色
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
CAS 數(shù)據(jù)庫52232-67-4(CAS DataBase Reference)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H227
WGK Germany3
WGK Germany3
海關編碼2937190000
毒害物質數(shù)據(jù)52232-67-4(Hazardous Substances Data)

常見問題列表

分子結構
特立帕肽是一種合成的34肽,為人甲狀旁腺素PTH的1-34氨基酸片段,該片段是含有84個氨基酸的內源性甲狀旁腺素PTH具有生物活性的N-末端區(qū)域。本品的免疫學和生物學特性與內源性甲狀旁腺素PTH以及牛甲狀旁腺素PTH(bPTH)完全相同。
藥代動力學

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,達峰時間(tmax)為30 min,半衰期(t1/2 )為60 min,靜脈注射血清半衰期為5 min,絕對生物利用度95%。90%藥物經(jīng)腎臟清除。

不良反應與安全性

特立帕肽注射后常見不良反應包括頭暈、背痛、惡心和下肢痙攣等,多為一過性;少見的不良反應包括心律失常、耳聾等。目前認為不良反應發(fā)生與患者年齡和給藥劑量之間無明顯關系。

作用機制
特立帕肽可通過抑制成骨細胞凋亡、激活骨襯細胞和增強成骨細胞分化來介導骨代謝。通過調節(jié)腺苷酸環(huán)化酶-環(huán)磷酸腺苷-蛋白激酶A傳導通路間歇性刺激成骨細胞、骨襯細胞和骨髓基質干細胞表面PHT-Ⅰ受體,促進成骨細胞的分化、延長成骨細胞壽命;通過磷酸酯C-胞漿鈣離子-蛋白激酶C信號傳導通路,刺激成骨細胞系增殖;通過抑制PPARγ的反式激活活性,減少基質細胞向脂肪細胞系分化,使成骨細胞數(shù)量增加;通過調節(jié)細胞因子間接調節(jié)骨的成長,例如可以誘導iGF-1與成骨細胞結合,從而促進骨的形成;通過Wnt信號通路調節(jié)骨形成的過程,從而增加骨的形成。
多肽類藥物
禮來公司甲狀旁腺激素復泰奧(特立帕肽)最早批準用于絕經(jīng)后婦女骨質疏松 癥,初期或性腺機能減退的男性骨質疏松癥患者,后來再次增加新適應癥用于 在具有骨折高風險的治療與持久性、全身性糖皮質激素治療有關的骨質疏松。
2011年復泰奧(特立帕肽)在全球銷售額達到9.51億美元。在中國市場,2011 年由禮來(法國)公司開始進口。
生物活性
Teriparatide (Human parathyroid hormone-(1-34)) 是 PHT 的激動劑,其在 HEK293 細胞中的 IC50 值為 2 nM。
靶點

IC50: 2 nM (PTH).

體內研究

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.

醋酸特立帕肽價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/11XW5223267401醋酸特立帕肽52232-67-425MG2748元
2024/01/16P1033Teriparatide Acetate52232-67-410mg1392.3元
2024/01/16P1033醋酸特立帕肽
Teriparatide Acetate
52232-67-450mg4176.9元
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