Tadalafil (IC351) - Moligand™, 10mM in DMSO , Phosphodiesterase 5A inhibitor, CAS No.171596-29-5, Phosphodiesterase 5A inhibitor

CAS: 171596-29-5 Cat. No.: T407959 Molecular Weight: 389.4 EC Number: 687-782-2 PubChem CID: 110635

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R,12aR)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Tadalafil (IC351) is aPDE-5inhibitor withIC50of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibitsPDE11
In vitro

Tadalafil binds to PDE5 with K_D of 2.4 nM. cGMP stimulates the binding of [³H]Tadalafil. Tadalafil (1 mM) results increased CYP3A protein expression in human hepatocytes.

In vivo

Tadalafil (2 mg/kg) almost completely restores penile oxygenation and abolishes neurotomy induced increase and substantially rescues muscle/fiber ratio in penile sectionsin sham-operated rats. Tadalafil (2 mg/kg or 10 mg/kg) significantly improves neurological functional recovery and increases cerebral vascular density and the percentage of BrdU-positive endothelial cells around the ischemic boundary. Tadalafil selectively increases cGMP but not cAMP in brain of rats. Tadalafil decreases the number of apoptotic cells and increases the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2 in mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

Pyrazino[1', 2':1, 6]pyrido[3, 4-b]indole-1, 4-dione, 6-(1, 3-benzodioxol-5-yl)-2, 3, 6, 7, 12, 12a-hexahydro-2-methyl-, (6R, 12aR)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Tadalafil (IC351) is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Phosphodiesterase 5A inhibitor

Product Properties

• ALogP: 2.3

Names and Identifiers

• Isomeric SMILES: CN1CC(=O)N2[C@@H](C1=O)CC3=C([C@H]2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36
• WGK Germany: 2
• RTECS: UQ4431050
• PubChem CID: 110635
• Molecular Weight: 389.4

Associated Targets(Human)

PDE11A Tchem Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (10 Activities)

Discover Target: PDE11A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE5A Tclin cGMP-specific 3',5'-cyclic phosphodiesterase (18 Activities)

Discover Target: PDE5A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE6C Tclin Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (1 Activities)

Discover Target: PDE6C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 4 mg/mL (10.82 mM); Water: Insoluble; Ethanol: Insoluble
• Flash Point(°F): 35.6 °F
• Flash Point(°C): 35.6°F

References

1. Qiang Huang, Zhiren Zou, Xiaobo Li, Qinwen Xiao, Guang Liang, Wenqi Wu.  (2023)  Poly (amino acid)s as new co-formers in amorphous solid dispersion.  INTERNATIONAL JOURNAL OF PHARMACEUTICS,      [PMID:36706970] [10.1016/j.ijpharm.2023.122645]

2. Wu Pan, Huiyun Xiao, Haizhu Li, Yongrui Li, Bin Zhang, Bowen Liu, Longliang Yang.  (2022)  Terahertz spectroscopic detection of antifatigue illegal additives in health care product matrices.  APPLIED OPTICS,  61  (33): (9904-9910).  [PMID:36606822] [10.1364/AO.462727]

3. Ting-Ting ZOU, Jin-Yi YANG, Zhen-Lin XU, Hong WANG, Yuan-Ming SUN, Hong-Tao LEI, Xue-Cai TAN, Yu-Dong SHEN.  (2019)  Detection of Tadalafil and Its Analogues in Health Wine and Oral Liquid by Microwell Lateral Flow Immunochromatography Assay.  CHINESE JOURNAL OF ANALYTICAL CHEMISTRY,      [PMID:] [10.1016/S1872-2040(19)61182-5]

4. Changzheng Xin, ShanShan Gao, Yaxin Din, Yanju Wu, Fei Wang.  (2019)  Direct Electrodeposition to Fabricate 3D Graphene Network Modified Glassy Carbon Electrode for Sensitive Determination of Tadalafil.  NANO,      [PMID:] [10.1142/S1793292019500097]

5. Fan He, Tingting Zou, Jinyi Yang, Hong Wang, Lihua Deng, Yuanxin Tian, Zhenlin Xu, Yuanming Sun, Hongtao Lei, Xuecai Tan, Yudong Shen.  (2019)  Development of a skeleton-specific antibody and Au nanoparticle-based immunochromatographic sensor for simultaneous detection of various tadalafil adulterants in health food.  FOOD AND AGRICULTURAL IMMUNOLOGY,      [PMID:] [10.1080/09540105.2019.1585417]

6. Xianzhi Liu, Luyan Shen, Lin Zhou, Wencheng Wu, Guang Liang, Yunjie Zhao, Wenqi Wu.  (2024)  Nucleotides as new co-formers in co-amorphous systems: Enhanced dissolution rate, water solubility and physical stability.  EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,      [PMID:38768766] [10.1016/j.ejpb.2024.114333]

7. Miao Tang, Yu Xin, Yunchun Zhao, Xiao Zhang, Meng Zhang, Dongli Sun, Xiaojun Zhu, Yao Yao, Weidong Fei, Caihong Zheng.  (2024)  Placenta-anchored tadalafil liposomes rescues intrauterine growth restriction through continuous placental blood perfusion improvement.  JOURNAL OF CONTROLLED RELEASE,      [PMID:38452820] [10.1016/j.jconrel.2024.03.004]