Nortadalafil
- CAS NO.:171596-36-4
- Empirical Formula: C21H17N3O4
- Molecular Weight: 375.38
- MDL number: MFCD19443817
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:12
What is Nortadalafil?
The Uses of Nortadalafil
A N-desmethyl analogue of the human PDE5 inhibitor Tadalafil (T004500). A potential antiplasmodial drug.
Biological Activity
the cgmp-specific pde5 is the major pde isozyme in the corpus cavernosum, and controls penile erection. the pde5 inhibitors used in the clinic amplify the no-ccmp pathway and enhance the normal process leading to penile erection.nortadalafil is demethyl tadalafil, which is a pde5 inhibitor currently marketed in pill form for treating erectile dysfunction under the name cialis and for the treatment of pulmonary arterial hypertension under the name adcirca.
in vitro
tadalafil has been identified as a highly potent pde5 inhibitor (ic50 = 5 nm) with high selectivity for pde5 vs pde1-4 and pde6. it displays 85-fold greater selectivity vs pde6 than sildenafil [1].
in vivo
tadalafil showed profound and long-lasting blood pressure lowering activity (30 mmhg/>7 h) in the spontaneously hypertensive rat model after oral administration (5 mg/kg) [1].
References
[1] daugan a, grondin p, ruault c, le monnier de gouville ac, coste h, linget jm, kirilovsky j, hyafil f, labaudinière r. the discovery of tadalafil: a novel and highly selective pde5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues. j med chem. 2003;46(21):4533-42.
[2] porst h, hell-momeni k, büttner h. chronic pde-5 inhibition in patients with erectile dysfunction - a treatment approach using tadalafil once-daily. expert opin pharmacother. 2012 jul;13(10):1481-94. doi: 10.1517/14656566.2012.693162.
Properties of Nortadalafil
Melting point: | 285-290℃ (methanol ) |
Boiling point: | 718.6±60.0 °C(Predicted) |
Density | 1.55±0.1 g/cm3(Predicted) |
storage temp. | Inert atmosphere,Room Temperature |
solubility | DMSO (Slightly), Methanol (Slightly, Sonicated) |
form | Solid |
pka | 13.53±0.40(Predicted) |
color | White to Pale Yellow |
Safety information for Nortadalafil
Signal word | Danger |
Pictogram(s) |
Corrosion Corrosives GHS05 Exclamation Mark Irritant GHS07 Environment GHS09 |
GHS Hazard Statements |
H314:Skin corrosion/irritation H317:Sensitisation, Skin H410:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P260:Do not breathe dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P272:Contaminated work clothing should not be allowed out of the workplace. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P391:Collect spillage. Hazardous to the aquatic environment P301+P330+P331:IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. P303+P361+P353:IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. P333+P313:IF SKIN irritation or rash occurs: Get medical advice/attention. P405:Store locked up. |
Computed Descriptors for Nortadalafil
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