PD 135158

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525842

CAS#: 130325-35-8

Description: PD 135158 is a Selective cholecystokinin type B (CCKB)/gastrin receptor agonist. In studies, PD- 135158 stimulates lipase release from isolated rat pancreatic acini dose dependently in a biphasic manner, with identical efficacy but lower potency compared to cholecystokinin octapeptide (CCK-8). PD 135158 is classified into Anti-Anxiety Agents, Central Nervous System Agents, Central Nervous System Depressants, Psychotropic Drugs, and Tranquilizing Agents.

Chemical Structure

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PD 135158
CAS# 130325-35-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525842
Name: PD 135158
CAS#: 130325-35-8
Chemical Formula: C42H61N5O11
Exact Mass: 811.44
Molecular Weight: 811.961
Elemental Analysis: C, 62.13; H, 7.57; N, 8.63; O, 21.68

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Cam 1028; Cam-1028; Cam1028; PD-135158; PD135158; PD 135158

IUPAC/Chemical Name: (2S,3R,4R,5R)-2,3,4,5,6-pentahydroxy-N-methylhexan-1-aminium 4-(((1S)-2-((2S)-3-(1H-indol-3-yl)-2-methyl-2-(((((2S)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)oxy)carbonyl)amino)propanamido)-1-phenylethyl)amino)-4-oxobutanoate

InChi Key: CWJXTOIDFOBOKQ-YCSHSMMXSA-N

InChi Code: InChI=1S/C35H44N4O6.C7H17NO5/c1-33(2)24-16-17-34(33,3)28(18-24)45-32(44)39-35(4,19-23-20-36-26-13-9-8-12-25(23)26)31(43)37-21-27(22-10-6-5-7-11-22)38-29(40)14-15-30(41)42;1-8-2-4(10)6(12)7(13)5(11)3-9/h5-13,20,24,27-28,36H,14-19,21H2,1-4H3,(H,37,43)(H,38,40)(H,39,44)(H,41,42);4-13H,2-3H2,1H3/t24?,27-,28+,34?,35+;4-,5+,6+,7+/m10/s1

SMILES Code: O[C@H]([C@H]([C@@H]([C@@H](CO)O)O)O)C[NH2+]C.O=C([O-])CCC(N[C@@H](C1=CC=CC=C1)CNC([C@](NC(O[C@@H]2C(C3(C)C)(C)CCC3C2)=O)(C)CC4=CNC5=C4C=CC=C5)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: PD 135158 is a Selective cholecystokinin type B (CCKB)/gastrin receptor agonist.
In vitro activity: Both lamotrigine and the mu-opioid agonist DAMGO inhibited mustard oil-evoked cell firing by approximately 50% compared with control levels. Co-application of CCK8S reversed DAMGO-, but not lamotrigine-induced inhibition of cell firing and this reversal was prevented with the selective CCK(B) receptor antagonist PD 135158. Reference: Neurosci Res. 2001 Apr;39(4):385-90. https://pubmed.ncbi.nlm.nih.gov/11274737/
In vivo activity: The present study examined the effects of the selective CCK(B) antagonist PD-135,158 (0.001, 0. 01, and 0.1 mg/kg) using a conditioned suppression of drinking procedure in rats. For purposes of comparison the effects of haloperidol (0.1 mg/kg) were also investigated. PD-135,158 (0.1 mg/kg), similar to haloperidol (0.1 mg/kg), elicited a clear LI effect under conditions that did not lead to LI in control rats (low number of preexposures). Reference: Pharmacol Biochem Behav. 2000 Mar;65(3):459-63. https://pubmed.ncbi.nlm.nih.gov/10683486/

Preparing Stock Solutions

The following data is based on the product molecular weight 811.96 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Blackburn-Munro G, Dickinson T, Fleetwood-Walker SM. Non-opioid actions of lamotrigine within the rat dorsal horn after inflammation and neuropathic nerve damage. Neurosci Res. 2001 Apr;39(4):385-90. doi: 10.1016/s0168-0102(00)00239-x. PMID: 11274737. 2. Gracey DJ, Bell R, King DJ. PD-135,158, a cholecystokinin(B) antagonist, enhances latent inhibition in the rat. Pharmacol Biochem Behav. 2000 Mar;65(3):459-63. doi: 10.1016/s0091-3057(99)00227-0. PMID: 10683486. 3. Tsutsumi T, Akiyoshi J, Isogawa K, Kohno Y, Hikichi T, Nagayama H. Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides. 1999 Dec;33(6):483-6. doi: 10.1054/npep.1999.0766. PMID: 10657528.
In vitro protocol: 1. Blackburn-Munro G, Dickinson T, Fleetwood-Walker SM. Non-opioid actions of lamotrigine within the rat dorsal horn after inflammation and neuropathic nerve damage. Neurosci Res. 2001 Apr;39(4):385-90. doi: 10.1016/s0168-0102(00)00239-x. PMID: 11274737.
In vivo protocol: 1. Gracey DJ, Bell R, King DJ. PD-135,158, a cholecystokinin(B) antagonist, enhances latent inhibition in the rat. Pharmacol Biochem Behav. 2000 Mar;65(3):459-63. doi: 10.1016/s0091-3057(99)00227-0. PMID: 10683486. 2. Tsutsumi T, Akiyoshi J, Isogawa K, Kohno Y, Hikichi T, Nagayama H. Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides. 1999 Dec;33(6):483-6. doi: 10.1054/npep.1999.0766. PMID: 10657528.

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1: Josselyn SA, Franco VP, Vaccarino FJ. PD-135158, a CCKB receptor antagonist, microinjected into the nucleus accumbens and the expression of conditioned rewarded behavior. Neurosci Lett. 1996 May 10;209(2):85-8. PubMed PMID: 8761988.
2: Höcker M, Hughes J, Fölsch UR, Schmidt WE. PD 135158, a CCKB/gastrin receptor antagonist, stimulates rat pancreatic enzyme secretion as a CCKA receptor agonist. Eur J Pharmacol. 1993 Sep 21;242(1):105-8. PubMed PMID: 7901038.