リオシグアット

化学名:リオシグアット

英語名:Riociguat

CBNumberCB62473752

MFC20H19FN8O2

MW422.42

别名

リオシグアット

リオシグアト

リオシグアト (JAN)

リオシグアット物理性質

融点	247-251°C (dec.)
沸点	567.2±50.0 °C(Predicted)
比重(密度)	1.51
貯蔵温度	Refrigerator
溶解性	DMSO（微加熱）、メタノール（微加熱）
酸解離定数(Pka)	1.51±0.50(Predicted)
外見	個体
色	オフホワイトからオレンジ
InChI	InChI=1S/C20H19FN8O2/c1-28(20(30)31-2)15-16(22)25-18(26-17(15)23)14-12-7-5-9-24-19(12)29(27-14)10-11-6-3-4-8-13(11)21/h3-9H,10H2,1-2H3,(H4,22,23,25,26)
InChIKey	WXXSNCNJFUAIDG-UHFFFAOYSA-N
SMILES	C(OC)(=O)N(C1=C(N)N=C(C2C3=CC=CN=C3N(CC3=CC=CC=C3F)N=2)N=C1N)C

危険有害性情報のコード(GHS)

用途
希少疾病用医薬品慢性血栓寒栓性肺高血圧症の治療
効能
血管拡張薬, グアニル酸シクラーゼ活性薬
商品名
アデムパス (バイエル薬品)
説明
In September 2013, Health Canada approved riociguat (also referred to as BAY 63-2521), for the treatment of patients with chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or inoperable CTEPH and for the treatment of adults with pulmonary arterial hypertension (PAH). Riociguat has a dual mode of action and works by (a) sensitizing sGC to the body’s NO by stabilizing NO–sGC binding and (b) an NO-independent, direct stimulation of sGC via a different binding site. This process restores the NO–sGC–cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.
Headache, dizziness, dyspepsia/gastritis, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation were the most common adverse events ( 3%) observed during riociguat clinical trials. Riociguat comes with a black box warning for embryo-fetal toxicity.
化学的特性
Brownish Orange Solid
使用
Riociguat is used in the treatment for pulmonary hypertension.
定義
ChEBI: A carbamate ester that is the methyl ester of {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamic acid. It is used for treatment of chronic thromboembolic pulmonary hypertension an pulmonary arterial hypertension