Ingredient Details :[(1S,2R,3R,4R,5R,6S,7S,8R,9R,10R,13R,14R,16S,17S,18R)-5,7,14-trihydroxy-6,8,16,18-tetramethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] benzoate


TCMI-ID: TCMI21960


Physicochemical Property
Ingredient Name [(1S,2R,3R,4R,5R,6S,7S,8R,9R,10R,13R,14R,16S,17S,18R)-5,7,14-trihydroxy-6,8,16,18-tetramethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] benzoate
Pubchem CID 102375480
Iupac name [(1S,2R,3R,4R,5R,6S,7S,8R,9R,10R,13R,14R,16S,17S,18R)-5,7,14-trihydroxy-6,8,16,18-tetramethoxy-13-(methoxymethyl)-11-methyl-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-4-yl] benzoate
Molecular Formula C32H45NO10
Molecular Weight 603.7
Isomeric smiles CN1C[C@@]2([C@@H](C[C@@H]([C@@]34[C@@H]2[C@H]([C@@H]([C@H]31)[C@@]5([C@@H]6[C@H]4C[C@@]([C@@H]6OC(=O)C7=CC=CC=C7)([C@H]([C@@H]5O)OC)O)OC)OC)OC)O)COC
InChI InChI=1S/C32H45NO10/c1-33-14-29(15-38-2)18(34)12-19(39-3)31-17-13-30(37)26(43-28(36)16-10-8-7-9-11-16)20(17)32(42-6,25(35)27(30)41-5)21(24(31)33)22(40-4)23(29)31/h7-11,17-27,34-35,37H,12-15H2,1-6H3/t17-,18-,19+,20-,21+,22+,23-,24-,25+,26-,27+,29+,30-,31+,32-/m1/s1
InChIKey GPKLKIFNFCDMHE-BMTFSNIDSA-N
External Database Links HERB2.0: HBIN029452  
Structural Information
nHA(Number of hydrogen bond acceptors) 11
nHD(Number of hydrogen bond donors) 3
nRot(Number of rotatable bonds) 9
nRing(Number of rings) 7
MaxRing(Number of atoms in the biggest ring) 6
nHet(Number of heteroatoms) 11

Stability
nRig(Number of rigid bonds) 31
Flexibility 0.29
Stereo Centers(Number of stereocenters) 15

Solubility
TPSA(Topological polar surface area) 136.38
logS(The logarithm of aqueous solubility value) -3.696
logP(The logarithm of the n-octanol/water distribution coefficient) 1.251
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 1.627

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.355
Synthetic accessibility score 7.265
Natural Product-likeness score 3.078
Lipinski Rule Rejected
GSK Rule Rejected
Golden Triangle Rejected

Absorption
Caco-2 Permeability -5.411
MDCK Permeability 6.94E-05
Pgp-substrate 0.991
HIA(human intestinal absorption) 0.748
F20%(20% Oral Bioavailability) 0.278
F30%(30% Oral Bioavailability) 0.743

Distribution
PPB(Plasma protein binding) 23.02%
VD(Volume Distribution) 0.751
BBB Penetration(Blood brain barrier penetration) 0.085
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 53.58%

Metabolism
CYP1A2 inhibitor 0.008
CYP1A2 substrate 0.962
CYP2C19 inhibitor 0.003
CYP2C19 substrate 0.762
CYP2C9 inhibitor 0.002
CYP2C9 substrate 0.011
CYP2D6 inhibitor 0.01
CYP2D6 substrate 0.322
CYP3A4 inhibitor 0.138
CYP3A4 substrate 0.53

Excretion
CL(The clearance of a drug) 4.136
T1/2 0.602

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.435

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.19
IGC50 3.603
LC50FM 4.953
LC50DM 8.203

Reproductive Effects
NR-AR(Androgen receptor) 0.084
NR-AR-LBD(Androgen receptor) 0.072
NR-Aromatase 0.211
NR-ER(Estrogen receptor) 0.098
NR-ER-LBD(Estrogen receptor) 0.115

Allergy
Skin Sensitization Rule 0
Skin Sensitization 0.151

Acute Toxicity
Acute Toxicity Rule 0
Rat Oral Acute Toxicity 0.627

Organ Toxicity
hERG Blockers 0.769
H-HT(The human hepatotoxicity) 0.891
DILI(Drug-induced liver injury) 0.35

Primary Irritation
Eye Corrosion 0.003
Eye Irritation 0.008
Respiratory Toxicity 0.944

Mutagenic Effects
AMES Toxicity 0.029

Tumorigenic Effects
Carcinogencity 0.006
SR-ARE(Antioxidant Response Element) 0.041
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.455
SR-p53 0.76

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