Tìm theo
Cilastatin
Các tên gọi khác (6 ) :
  • (L)-7-(2-Amino-2-carboxy-ethylsulfanyl)-2-[(2,2-dimethyl-cyclopropanecarbonyl)-amino]-hept-2-enoic acid
  • (Z)-(S)-6-Carboxy-6-[(S)-2,2-dimethylcyclopropanecarboxamido]hex-5-enyl-L-cysteine
  • (Z)-7-((R)-2-Amino-2-carboxy-ethylsulfanyl)-2-[((S)-2,2-dimethyl-cyclopropanecarbonyl)-amino]-hept-2-enoic acid
  • Cilastatina
  • Cilastatine
  • Cilastatinum
Thuốc Gốc
Small Molecule
CAS: 82009-34-5
CTHH: C16H26N2O5S
PTK: 358.453
A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H26N2O5S
Phân tử khối
358.453
Monoisotopic mass
358.156242642
InChI
InChI=1S/C16H26N2O5S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23)/b12-6-/t10-,11+/m1/s1
InChI Key
InChIKey=DHSUYTOATWAVLW-WFVMDLQDSA-N
IUPAC Name
(2Z)-7-{[(2R)-2-amino-2-carboxyethyl]sulfanyl}-2-{[(1S)-2,2-dimethylcyclopropyl]formamido}hept-2-enoic acid
Traditional IUPAC Name
cilastatin
SMILES
N[C@@H](CSCCCC\C=C(/NC(=O)[C@H]1CC1(C)C)C(=O)O)C(=O)O
Độ hòa tan
1.00e-01 g/l
logP
-1.3
logS
-3.5
pKa (strongest acidic)
2.53
pKa (Strongest Basic)
9.14
PSA
129.72 Å2
Refractivity
92.85 m3·mol-1
Polarizability
38.28 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
6
H Bond Donor Count
4
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Cilastatin is a chemical compound which inhibits the human enzyme dehydropeptidase. Dehydropeptidase is found in the kidney and is responsible for degrading the antibiotic imipenem. Cilastatin is therefore combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect. However, cilastatin in and of itself does not have any antibacterial activity.
Cơ Chế Tác Dụng : A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4. [PubChem] Cilastatin is a specific and reversible renal dehydropeptidase-I inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to block the metabolism and thus the inactivation of imipenem so that antibacterial levels of imipenem can be attained in the urine. The drug also prevents the metabolism of leukotriene D4 to leukotriene E4 through the inhibition of leukotriene D4 dipeptidase.
Chỉ Định : Combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect.
Tương Tác Thuốc :
  • Cyclosporine Imipenem increases the effect and toxicity of cyclosporine
  • Valganciclovir Generalized convulsions have been reported in patients taking Ganciclovir and Imipenem-cilastatin. Concomitant therapy should be avoided. (Note: Valganciclovir is converted to Ganciclovir in vivo)
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01597
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6435415
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505611
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C01675
ChemSpider
http://www.chemspider.com/Chemical-Structure.4444109.html
PharmGKB
http://www.pharmgkb.org/drug/PA448998
Wikipedia
http://en.wikipedia.org/wiki/Cilastatin
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