Ingredient Details :(2R,3R,4R,5R,6S,7S,8R,13S,14R,16S,18R)-11-ethyl-6,16,18-trimethoxy-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-4,5,7,8,14-pentol


TCMI-ID: TCMI22225


Physicochemical Property
Ingredient Name (2R,3R,4R,5R,6S,7S,8R,13S,14R,16S,18R)-11-ethyl-6,16,18-trimethoxy-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-4,5,7,8,14-pentol
Pubchem CID 122173269
Iupac name (2R,3R,4R,5R,6S,7S,8R,13S,14R,16S,18R)-11-ethyl-6,16,18-trimethoxy-13-(methoxymethyl)-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecane-4,5,7,8,14-pentol
Molecular Formula C25H41NO9
Molecular Weight 499.6
Isomeric smiles CCN1C[C@]2([C@@H](C[C@@H](C34C2[C@H](C(C31)[C@@]5([C@@H]6[C@H]4C[C@@]([C@@H]6O)([C@H]([C@@H]5O)OC)O)O)OC)OC)O)COC
InChI InChI=1S/C25H41NO9/c1-6-26-9-22(10-32-2)12(27)7-13(33-3)24-11-8-23(30)19(28)14(11)25(31,20(29)21(23)35-5)15(18(24)26)16(34-4)17(22)24/h11-21,27-31H,6-10H2,1-5H3/t11-,12-,13+,14-,15?,16+,17?,18?,19-,20+,21+,22-,23-,24?,25-/m1/s1
InChIKey SQMGCPHFHQGPIF-JPTXIPOMSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 10
nHD(Number of hydrogen bond donors) 5
nRot(Number of rotatable bonds) 6
nRing(Number of rings) 6
MaxRing(Number of atoms in the biggest ring) 0
nHet(Number of heteroatoms) 10

Stability
nRig(Number of rigid bonds) 24
Flexibility 0.25
Stereo Centers(Number of stereocenters) 15

Solubility
TPSA(Topological polar surface area) 141.31
logS(The logarithm of aqueous solubility value) -3.619
logP(The logarithm of the n-octanol/water distribution coefficient) 0.19
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) -0.067

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.285
Synthetic accessibility score 7.476
Natural Product-likeness score 3.313
Lipinski Rule Accepted
GSK Rule Rejected
Golden Triangle Accepted

Absorption
Caco-2 Permeability -5.835
MDCK Permeability 8.50E-05
Pgp-substrate 0.995
HIA(human intestinal absorption) 0.884
F20%(20% Oral Bioavailability) 0.093
F30%(30% Oral Bioavailability) 0.93

Distribution
PPB(Plasma protein binding) 19.29%
VD(Volume Distribution) 0.458
BBB Penetration(Blood brain barrier penetration) 0.069
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 63.95%

Metabolism
CYP1A2 inhibitor 0.001
CYP1A2 substrate 0.953
CYP2C19 inhibitor 0.001
CYP2C19 substrate 0.686
CYP2C9 inhibitor 0
CYP2C9 substrate 0.012
CYP2D6 inhibitor 0.001
CYP2D6 substrate 0.216
CYP3A4 inhibitor 0.01
CYP3A4 substrate 0.08

Excretion
CL(The clearance of a drug) 1.868
T1/2 0.445

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.252

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.231
IGC50 2.41
LC50FM 2.625
LC50DM 7.724

Reproductive Effects
NR-AR(Androgen receptor) 0.04
NR-AR-LBD(Androgen receptor) 0.033
NR-Aromatase 0.042
NR-ER(Estrogen receptor) 0.123
NR-ER-LBD(Estrogen receptor) 0.241

Allergy
Skin Sensitization Rule 0
Skin Sensitization 0.44

Acute Toxicity
Acute Toxicity Rule 0
Rat Oral Acute Toxicity 0.457

Organ Toxicity
hERG Blockers 0.356
H-HT(The human hepatotoxicity) 0.407
DILI(Drug-induced liver injury) 0.019

Primary Irritation
Eye Corrosion 0.003
Eye Irritation 0.005
Respiratory Toxicity 0.976

Mutagenic Effects
AMES Toxicity 0.104

Tumorigenic Effects
Carcinogencity 0.01
SR-ARE(Antioxidant Response Element) 0.023
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.637
SR-p53 0.551

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