Tìm theo
Pirfenidone
Thuốc Gốc
Small Molecule
CAS: 53179-13-8
CTHH: C12H11NO
PTK: 185.2218
Pirfenidone is an orally active small molecule drug that may inhibit collagen synthesis, down regulate production of multiple cytokines and block fibroblast proliferation and stimulation in response to cytokines. Pirfenidone has demonstrated activity in multiple fibrotic conditions, including those of the lung, kidney and liver. It is being investigated by InterMune.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H11NO
Phân tử khối
185.2218
Monoisotopic mass
185.084063979
InChI
InChI=1S/C12H11NO/c1-10-7-8-12(14)13(9-10)11-5-3-2-4-6-11/h2-9H,1H3
InChI Key
InChIKey=ISWRGOKTTBVCFA-UHFFFAOYSA-N
IUPAC Name
5-methyl-1-phenyl-1,2-dihydropyridin-2-one
Traditional IUPAC Name
pirfenidone
SMILES
CC1=CN(C(=O)C=C1)C1=CC=CC=C1
Độ hòa tan
2.89e+00 g/l
logP
2.14
logS
-1.8
pKa (Strongest Basic)
-1.2
PSA
20.31 Å2
Refractivity
57 m3·mol-1
Polarizability
20.28 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pirfenidone is a novel agent with anti-inflammatory, antioxidant, and antifibrotic properties. It may improve lung function and reduce the number of acute exacerbations in patients with idiopathic pulmonary fibrosis (IPF).
Cơ Chế Tác Dụng : Pirfenidone is an orally active small molecule drug that may inhibit collagen synthesis, down regulate production of multiple cytokines and block fibroblast proliferation and stimulation in response to cytokines. Pirfenidone has demonstrated activity in multiple fibrotic conditions, including those of the lung, kidney and liver. It is being investigated by InterMune. Pirfenidone is an orally active, small molecule that shows a wide range of biologic activity. In vitro evidence has shown that pirfenidone inhibits collagen synthesis, down-regulates profibrotic cytokines and decreases fibroblast proliferation. Pirfenidone leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin. In addition, pirfenidone reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-beta target gene and furin substrate involved in carcinogenesis.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration.
▧ Half Life :
2-2.5 hours
Độc Tính : Generally well tolerated with the most frequent side effects reported being photosensitivity rash and gastrointestinal symptoms.
Chỉ Định : For the treatment of idiopathic pulmonary fibrosis (IPF).
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04951
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=40632
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=11111619
ChemSpider
http://www.chemspider.com/Chemical-Structure.37115.html
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