Risedronate Sodium

HCID 4194514

기본 정보

CAS
115436-72-1
표준 SMILES
O=P([O-])(O)C(O)(Cc1cccnc1)P(=O)(O)O.[Na+]
InChIKey
DRFDPXKCEWYIAW-UHFFFAOYSA-M
분자식
C7H10NNaO7P2
평균 분자량
305.09 g/mol
단동위원소 질량
304.98301994

개요

Risedronate sodium is a 1,1-bis(phosphonic acid).

이름 및 식별자

우선 이름
Risedronate Sodium
IUPAC
sodium hydroxy-(1-hydroxy-1-phosphono-2-pyridin-3-ylethyl)phosphinate
영어명
Sodium risedronate
분자식
C7H12NNaO7P2
분자량
307.11

이름 및 동의어

Risedronate sodium115436-72-1ActonelAtelviaRisedronate monosodiumRisedronic acid monosodium saltOFG5EXG60Lrisedronate sodium anhydrousNE-58095 ANHYDROUSNSC-722598NSC-759280Monosodium (1-hydroxy-2-(3-pyridinyl)ethylidene)bisphosphonate
이름 더 보기
NE 58095RISEDRONATE NArisedronate,RIDNE 58095 SodiumSodium risedroteRESIDROTE SODIUMRisedronat sodiumRISEDREMATE SODIUM
Phosphonic acid, (1-hydroxy-2-(3-pyridinyl)ethylidene)bis-, monosodium saltDTXCID9026132NSC722598Risendronate SodiumRefChem:930781Risedronate sodium hemi-pentahydrate; risedronate sodium monohydrate658-043-1DTXSID1046132

데이터베이스 식별자

CAS
115436-72-1、122458-82-6
PubChem CID
4194514
DTXSID
DTXSID20924178
ChEMBL
CHEMBL1654
ChEBI
CHEBI:8868
UNII
OFG5EXG60L
EC Number
601-362-8、658-043-1

물성

구조 계산 물성

극성 표면적
151 Ų
수소 결합 공여자 수
4
수소 결합 수용자 수
8
회전 가능 결합 수
4
무거운 원자 수
18

실험 및 물리화학적 성질

Human Drugs · 2건

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

물리화학적 성질

녹는점
252 · 252-262°C
저장 조건
room temp
용해도
2 O: · H2O: 용해성5mg/mL, 투명(따뜻한)
물리적 상태
가루
색상
흰색에서 베이지색
수용성
10 mM · Soluble to 10 mM in water

화학적 성질

Fine White to Off-White Crystalline Powder

안전 및 규제

GHS 분류

GHS Classification · 6건

Warning

H302+H312+H332 (86.4%): Harmful if swallowed, in contact with skin or if inhaled [Warning Acute toxicity, oral; acute toxicity, dermal; acute toxicity, inhalation]

P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P321, P330, P362+P364, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 44 reports by companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Danger

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

유해성 정보

Hazard Classes and CategoriesAcute Tox. 4 (93.2%)

독성 정보

Exposure RoutesRapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract
Toxicity Summary · 1건

The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

Signs and Symptoms · 1건

Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness.

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver Injury · 6건

Drug Induced Liver Injury Rank (DILIrank 2.0)

Risedronate sodium

Ambiguous-DILI-concern

3

Adverse reactions

DOI:10.1016/j.drudis.2016.02.015

안전 데이터

wgk
3
rtecs
SZ8567500
HS 번호
29333990
risk_code
62-64
safety_code
20-22-36/37
Hazard Classifications
Acute Tox. 4 DermalAcute Tox. 4 InhalationAcute Tox. 4 Oral

화학 및 산업

약리 정보

Metabolism/Metabolites · 1건

No evidence found for metabolization of risedronate in humans or mammals. Route of Elimination: Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats. Half Life: 1.5 hours

FDA Pharmacological Classification · 2건

RISEDRONATE SODIUM

Diphosphonates [CS]; Bisphosphonate [EPC]

MeSH Pharmacological Classification · 2건

A class of drugs that act by selective inhibition of calcium influx through cellular membranes.

Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS.

용도 및 제조

UsesFor the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis
응용 분야 · 2건

개요Risedronate sodium was launched as Actonel in the US for treatment of Paget's disease. Risedronic acid is readily obtained by condensation of 2-(3- pyridyl)acetic acid with phosphorous acid in presence of phosphorus oxychloride. Risedronate sodium is an orally active bisphosphonate of third generation, showing more potent bone antiresorptive properties than most of prior bisphosphonates like etidronate which has been used for the same indication since 1978. The biological mechanism by which Risedronate, and generally bisphosphonates, act is not quite clear presently ; recent advances have suggested that aminobisphosphonates interfere with the HMG-CoA pathway and inhibit protein prenylation, causing apoptosis of osteoclasts and macrophages. These apoptotic effects are correlated to the anti-resorptive properties of this class of compounds. In a 2 month clinical trial involving patients with Paget's desease, 30 mg risedronate daily achieved an appreciable reduction of serum alkaline phosphatase levels, an indicator of bone stabilization, in 77% of patients, compared with 11% on etidronate at 400 mg daily for 6 months. Risedronate is also in development for the treatment and prevention of various bone diseases, particularly post-menopausal and corticosteroid-induced osteoporosis.

용도Risedronic Acid is a pyridinyl biphosphonate bone resorption inhibitor.

공급사100 곳

北京华美互利生物化工010-56205725 · [email protected]
上海阿拉丁生化科技股份有限公司400-6206333 13167063860 · [email protected]
合肥翰刚医药科技有限公司+8618062405514 · [email protected]
河北展药生物科技有限公司15369953316 +8615369953316 · [email protected]
Dayang Chem (Hangzhou) Co.,Ltd.+86-0571-88938639 17705817739 · [email protected]

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