(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
- Product Name
- (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
- CAS No.
- 204067-01-6
- Chemical Name
- (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
- Synonyms
- PD 176252;PD176252, 10 mM in DMSO;(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE;(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE;(S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide;1H-Indole-3-propanamide, N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-, (αS)-
- CBNumber
- CB02453426
- Molecular Formula
- C32H36N6O5
- Formula Weight
- 584.67
- MOL File
- 204067-01-6.mol
(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE Property
- Boiling point:
- 838.8±65.0 °C(Predicted)
- Density
- 1.297±0.06 g/cm3(Predicted)
- storage temp.
- Store at +4°C
- solubility
- Soluble to 100 mM in DMSO
- form
- Powder
- pka
- 11.60±0.46(Predicted)
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 2602
- Product name
- PD176252
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $320
- Updated
- 2021/12/16
- Product number
- P218368
- Product name
- PD176252
- Packaging
- 10mg
- Price
- $335
- Updated
- 2021/12/16
- Product number
- 256190
- Product name
- PD 176252
- Packaging
- 10mg
- Price
- $573
- Updated
- 2021/12/16
- Product number
- CS-0027145
- Product name
- PD176252
- Purity
- >99.0%
- Packaging
- 5mg
- Price
- $70
- Updated
- 2021/12/16
- Product number
- CS-0027145
- Product name
- PD176252
- Purity
- >99.0%
- Packaging
- 10mg
- Price
- $110
- Updated
- 2021/12/16
(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE Chemical Properties,Usage,Production
Uses
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
Biological Activity
Non-peptide gastrin-releasing peptide receptor (GRP-R, BB 2 ) and neuromedin B receptor (NMB-R, BB 1 ) antagonist (K i values are 0.17 and 1.0 nM for BB 1 and BB 2 respectively). Inhibits proliferation of rat C6 glioma cells (IC 50 = 2 μ M) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC 50 = 5 μ M).
in vivo
PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice[3].
storage
Store at +4°C
References
[1] Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94. DOI:10.1016/s0960-894x(98)00462-4
[2] Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90. DOI:10.1124/mol.110.068288
[3] Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9. DOI:10.1016/s0014-2999(03)01996-4
(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE Preparation Products And Raw materials
Raw materials
Preparation Products
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