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阿仑膦酸钠,三水合物

阿仑膦酸钠,三水合物用途

Alendronate sodium hydrate 是一种 farnesyl diphosphate synthase 抑制剂,IC50 值为 460 nM。

阿仑膦酸钠,三水合物名称

[ CAS 号 ]:
121268-17-5

[ 中文名 ]:
阿仑膦酸钠

[ 英文名 ]:
Alendronate sodium

[中文别名 ]:

[英文别名 ]:

Alendronate sodium
Alendronate sodium trihydrate
Sodium Alendronate Trihydrate
alendronate sodium hydrate
Alendronate monosodium trihydrate
MFCD01748233
Alendronic acid monosodium salt trihydrate
onclast
Adronat
Dronal

阿仑膦酸钠,三水合物生物活性

[ 描述 ]:

Alendronate sodium hydrate 是一种 farnesyl diphosphate synthase 抑制剂,IC50 值为 460 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

[ 靶点 ]

IC50: 460 nM (farnesyl diphosphate synthase)

[体外研究]

阿仑膦酸盐直接作用于破骨细胞,抑制胆固醇生物合成途径中的限速步骤,这对于破骨细胞功能至关重要[1]。由于香叶基香叶基二磷酸酯水平降低,阿仑膦酸盐抑制类异戊二烯生物合成途径并干扰蛋白质异戊烯化。阿仑膦酸盐抑制[3H]甲羟戊酸内酯掺入18-25 kDa的蛋白质和不可皂化的脂质,包括破骨细胞中的甾醇[2]。阿仑膦酸盐引起[3H] MVA掺入甾醇的剂量依赖性抑制,并伴随着放射性标记掺入IPP和DMAPP的增加[3]。

[体内研究]

阿仑膦酸钠导致兔胃糜烂,但大鼠不会出现窦溃疡。阿仑膦酸盐增加吲哚美辛诱导的胃窦溃疡的发生率和大小。阿仑膦酸盐还可增强吲哚美辛诱导的大鼠胃损伤,延缓胃溃疡愈合[4]。阿仑膦酸盐(每周两次0.04-0.1mg/kg或每周0.1mg/kg)部分阻断人PC-3ML细胞的骨转移的建立,并导致腹膜和其他软组织中的肿瘤形成。阿仑膦酸盐预处理小鼠(每周两次或每周一次0.1 mg/kg)和紫杉醇(10-50 mg/kg /天,每周两次或每周一次)给药可阻断PC-3 ML肿瘤在骨髓和软组织中的生长组织以统计学上显着的方式显着提高存活率4-5周[5]。

[激酶实验]

大鼠肝细胞溶质由来自大鼠的单独肝脏制备。测定的总体积为0.1mL，含有10mg胞质蛋白和根据Rilling的组分。将所有反应组分（IPP除外）混合并在冰上保持15分钟。通过加入[14 C] IPP并在37℃温育来引发反应。 5分钟后，通过加入0.4mL MeOH / HCl（4/1，按体积计）终止反应，并将样品再孵育15分钟以将烯丙基焦磷酸酯水解成石油醚可提取产物。加入0.5mL水和1mL石油醚后，取50％上层（石油醚可萃取的）相进行液体闪烁分析。初步实验表明，在这些条件下，反应与时间和蛋白质呈线性关系，并且不超过10％的底物被消耗。

[参考文献]

[1]. Fisher JE, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8.

[2]. Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41.

[3]. Keller RK, et al. Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3.

[4]. Elliott SN, et al. Alendronate induces gastric injury and delays ulcer healing in rodents. Life Sci. 1998;62(1):77-91.

[5]. Stearns ME, et al. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion Metastasis. 1996;16(3):116-31.

[相关活性小分子]

阿仑膦酸钠,三水合物物理化学性质

[ 密度 ]:
1.857g/cm3

[ 沸点 ]:
616.7ºC at 760 mmHg

[ 熔点 ]:
245°C

[ 分子式 ]:
C₄H₁₈NNaO₁₀P₂

[ 分子量 ]:
325.124

[ 闪点 ]:
326.7ºC

[ 精确质量 ]:
325.030365

[ PSA ]:
211.45000

[ 外观性状 ]:
白色结晶固体

[ 储存条件 ]:
−20°C

[ 稳定性 ]:
Store in freezer

[ 水溶解性 ]:
water, double-distilled: 10 mg/mL

阿仑膦酸钠,三水合物MSDS

详细MSDS(安全技术说明书)

阿仑膦酸钠,三水合物毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SZ6523500

CHEMICAL NAME :: Phosphonic acid, (4-amino-1-hydroxybutylidene)bis-, monosodium salt, trihydrate

CAS REGISTRY NUMBER :: 121268-17-5

LAST UPDATED :: 199609

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C4-H13-N-O7-P2.3H2-O.Na

MOLECULAR WEIGHT :: 294.17

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 700 ug/kg/7D-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of esophagus Gastrointestinal - other changes

REFERENCE :: AJGAAR American Journal of Gastroenterology. (American College of Gastroenterology, Inc., 428 E. Preston St., Baltimore, MD 21202) V.21- 1954- Volume(issue)/page/year: 90,1889,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3229,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3229,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9100 ug/kg/13W-I

TOXIC EFFECTS :: Blood - pigmented or nucleated red blood cells Blood - changes in erythrocyte (RBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3244,1994 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 510 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating - 20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 121,217,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 42 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - other measures of fertility

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3319,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 27500 ug/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical Reproductive - Effects on Newborn - delayed effects

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3339,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 26 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical Reproductive - Effects on Newborn - delayed effects

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3373,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 650 ug/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3363,1994

阿仑膦酸钠,三水合物安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
R22:Harmful if swallowed. R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26:In case of contact with eyes, rinse immediately with plenty of water and seek medical advice . S36:Wear suitable protective clothing .

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
SZ6523500

[ 海关编码 ]:
29310095

阿仑膦酸钠,三水合物合成路线

详细合成路线

阿仑膦酸钠,三水合物上下游产品

阿仑膦酸钠,三水合物上游产品

阿仑膦酸钠,三水合物下游产品

阿仑膦酸钠,三水合物文献

Pharmacological inhibition of Dock5 prevents osteolysis by affecting osteoclast podosome organization while preserving bone formation.

Nat. Commun. 6 , 6218, (2015)

Osteoporosis is caused by excessive activity of bone-degrading osteoclasts over bone-forming osteoblast. Standard antiosteolytic treatments inhibit bone resorption by inducing osteoclast loss, with th...

Effects of aminobisphosphonates and thiazides in patients with osteopenia/osteoporosis, hypercalciuria, and recurring renal calcium lithiasis.

Urology 81(4) , 731-7, (2013)

To analyze the effects of aminobisphosphonates and thiazides on renal lithogenic activity and bone mineral density in patients with recurring renal calcium lithiasis.A prospective cohort study with 3 ...

Effect of alendronate on post-traumatic osteoarthritis induced by anterior cruciate ligament rupture in mice.

Arthritis. Res. Ther. 17 , 30, (2015)

Previous studies in animal models of osteoarthritis suggest that alendronate (ALN) has antiresorptive and chondroprotective effects, and can reduce osteophyte formation. However, these studies used no...

更多文献

阿仑膦酸钠,三水合物相关知识

阿仑膦酸钠片-说明书-副作用

2018-12-19 20:25:52

导读：阿仑膦酸钠是全球应用最广泛的抗骨质疏松药物，1993年就在美国上市，能显著增加患者骨密度、降低骨折风险，是骨质疏松一线治疗药物。阿仑膦酸钠为氨基二膦酸盐骨吸收抑制剂，与骨内羟磷灰石有强亲和力，能进入骨基质羟磷灰石晶体中，当破骨细胞溶解晶体，药物被释放，能抑制破骨细胞活性，并通过成骨细胞间接起...