Ingredient Details :2-[4-hydroxy-2-(hydroxymethyl)-6-[(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-piperidine]-16-yl]oxy-5-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol


TCMI-ID: TCMI11045


Physicochemical Property
Ingredient Name 2-[4-hydroxy-2-(hydroxymethyl)-6-[(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-piperidine]-16-yl]oxy-5-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol
Pubchem CID 5458956
Iupac name 2-[4-hydroxy-2-(hydroxymethyl)-6-[(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-piperidine]-16-yl]oxy-5-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol
Molecular Formula C45H73NO15
Molecular Weight 868.1
Isomeric smiles C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)C[C@@H]4[C@@]3(CC[C@H]5[C@H]4CC=C6[C@@]5(CC[C@@H](C6)OC7C(C(C(C(O7)CO)OC8C(C(C(C(O8)C)O)O)O)O)OC9C(C(C(C(O9)C)O)O)O)C)C)C)NC1
InChI InChI=1S/C45H73NO15/c1-19-9-14-45(46-17-19)20(2)30-28(61-45)16-27-25-8-7-23-15-24(10-12-43(23,5)26(25)11-13-44(27,30)6)57-42-39(60-41-36(53)34(51)32(49)22(4)56-41)37(54)38(29(18-47)58-42)59-40-35(52)33(50)31(48)21(3)55-40/h7,19-22,24-42,46-54H,8-18H2,1-6H3/t19-,20+,21?,22?,24+,25-,26+,27+,28+,29?,30+,31?,32?,33?,34?,35?,36?,37?,38?,39?,40?,41?,42?,43+,44+,45-/m1/s1
InChIKey MBWUSSKCCUMJHO-PUQINFEQSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 16
nHD(Number of hydrogen bond donors) 9
nRot(Number of rotatable bonds) 7
nRing(Number of rings) 9
MaxRing(Number of atoms in the biggest ring) 20
nHet(Number of heteroatoms) 16

Stability
nRig(Number of rigid bonds) 48
Flexibility 0.146
Stereo Centers(Number of stereocenters) 26

Solubility
TPSA(Topological polar surface area) 238.48
logS(The logarithm of aqueous solubility value) -2.408
logP(The logarithm of the n-octanol/water distribution coefficient) 2.396
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 3.03

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.161
Synthetic accessibility score 6.751
Natural Product-likeness score 2.384
Lipinski Rule Rejected
GSK Rule Rejected
Golden Triangle Rejected

Absorption
Caco-2 Permeability -5.975
MDCK Permeability 0.000171122
Pgp-substrate 0.068
HIA(human intestinal absorption) 0.995
F20%(20% Oral Bioavailability) 0.361
F30%(30% Oral Bioavailability) 0.996

Distribution
PPB(Plasma protein binding) 39.83%
VD(Volume Distribution) 0.081
BBB Penetration(Blood brain barrier penetration) 0.135
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 21.71%

Metabolism
CYP1A2 inhibitor 0
CYP1A2 substrate 0.138
CYP2C19 inhibitor 0.001
CYP2C19 substrate 0.339
CYP2C9 inhibitor 0
CYP2C9 substrate 0.031
CYP2D6 inhibitor 0.001
CYP2D6 substrate 0.143
CYP3A4 inhibitor 0.018
CYP3A4 substrate 0.056

Excretion
CL(The clearance of a drug) 0.575
T1/2 0.12

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.793

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.87
IGC50 3.628
LC50FM 4.873
LC50DM 5.397

Reproductive Effects
NR-AR(Androgen receptor) 0.003
NR-AR-LBD(Androgen receptor) 0.24
NR-Aromatase 0.057
NR-ER(Estrogen receptor) 0.236
NR-ER-LBD(Estrogen receptor) 0.354

Allergy
Skin Sensitization Rule 1
Skin Sensitization 0.041

Acute Toxicity
Acute Toxicity Rule 0
Rat Oral Acute Toxicity 0.197

Organ Toxicity
hERG Blockers 0.871
H-HT(The human hepatotoxicity) 0.251
DILI(Drug-induced liver injury) 0.022

Primary Irritation
Eye Corrosion 0.003
Eye Irritation 0.002
Respiratory Toxicity 0.972

Mutagenic Effects
AMES Toxicity 0.211

Tumorigenic Effects
Carcinogencity 0.426
SR-ARE(Antioxidant Response Element) 0.298
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.553
SR-p53 0.766

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