PZM21 featured

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MedKoo CAT#: 526831 CAS#: 1997387-43-5 (free base)

Description: PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potency and efficacy similar to morphine, but with less β-arrestin 2 recruitment. In tests on mice, PZM21 was slightly less potent than morphine or TRV130 as an analgesic, but also had significantly reduced adverse effects, with less constipation than morphine, and very little respiratory depression, even at high doses.

Price and Availability

Size Price Shipping out time Quantity 10mg USD 90 Same day 25mg USD 150 Same day 50mg USD 250 Same day 100mg USD 450 Same day 200mg USD 850 Same day 500mg USD 1850 Same day 1g USD 2950 Same day 2g USD 5250 Same day Inquire bulk and customized quantity Add to cart Pricing updated 2020-09-22. Prices are subject to change without notice.

Chemical Structure Theoretical Analysis MedKoo Cat#: 526831

Name: PZM21

CAS#: 1997387-43-5 (free base)

Chemical Formula: C19H27N3O2S

Exact Mass: 361.1824

Molecular Weight: 361.5

Elemental Analysis: C, 63.13; H, 7.53; N, 11.62; O, 8.85; S, 8.87

PZM21, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 1997387-43-5 (free base) 2287250-29-5 (HCl) 2287246-62-0 (sulfate)

Synonym: PZM21; PZM-21; PZM 21

IUPAC/Chemical Name: 1-[(2S)-2-(Dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea

InChi Key: MEDBIJOVZJEMBI-YOEHRIQHSA-N

InChi Code: InChI=1S/C19H27N3O2S/c1-14(10-16-8-9-25-13-16)21-19(24)20-12-17(22(2)3)11-15-4-6-18(23)7-5-15/h4-9,13-14,17,23H,10-12H2,1-3H3,(H2,20,21,24)/t14-,17-/m0/s1

SMILES Code: O=C(N[C@@H](C)CC1=CSC=C1)NC[C@@H](N(C)C)CC2=CC=C(O)C=C2

Technical Data

Appearance: White to off-white solid powder

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

Safety Data Sheet (SDS): View Safety Data Sheet (SDS)



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

References

1: Kudla L, Bugno R, Skupio U, Wiktorowska L, Solecki W, Wojtas A, Golembiowska K, Zádor F, Benyhe S, Buda S, Makuch W, Przewlocka B, Bojarski AJ, Przewlocki R. Functional characterization of a novel opioid, PZM21, and its influence on behavioural responses to morphine. Br J Pharmacol. 2019 Jul 26. doi: 10.1111/bph.14805. [Epub ahead of print] PubMed PMID: 31347704.

2: Yaksh TL, Eddinger KA, Kokubu S, Wang Z, DiNardo A, Ramachandran R, Zhu Y, He Y, Weren F, Quang D, Malkmus SA, Lansu K, Kroeze WK, Eliceiri B, Steinauer JJ, Schiller PW, Gmeiner P, Page LM, Hildebrand KR. Mast Cell Degranulation and Fibroblast Activation in the Morphine-induced Spinal Mass: Role of Mas-related G Protein-coupled Receptor Signaling. Anesthesiology. 2019 Jul;131(1):132-147. doi: 10.1097/ALN.0000000000002730. PubMed PMID: 31225809; PubMed Central PMCID: PMC6590697.

3: Yudin Y, Rohacs T. The G-protein-biased agents PZM21 and TRV130 are partial agonists of μ-opioid receptor-mediated signalling to ion channels. Br J Pharmacol. 2019 Sep;176(17):3110-3125. doi: 10.1111/bph.14702. Epub 2019 Jul 9. PubMed PMID: 31074038; PubMed Central PMCID: PMC6692666.

4: Ma M, Sun J, Li M, Yu Z, Cheng J, Zhong B, Shi W. Synthesis and Evaluation of Novel Biased μ-Opioid-Receptor (μOR) Agonists. Molecules. 2019 Jan 11;24(2). pii: E259. doi: 10.3390/molecules24020259. PubMed PMID: 30641969; PubMed Central PMCID: PMC6359544.

5: Araldi D, Ferrari LF, Levine JD. Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat. Neuroscience. 2018 Dec 1;394:60-71. doi: 10.1016/j.neuroscience.2018.10.015. Epub 2018 Oct 17. PubMed PMID: 30342200; PubMed Central PMCID: PMC6261666.

6: Zhu L, Cui Z, Zhu Q, Zha X, Xu Y. Novel Opioid Receptor Agonists with Reduced Morphine-like Side Effects. Mini Rev Med Chem. 2018;18(19):1603-1610. doi: 10.2174/1389557518666180716124336. Review. PubMed PMID: 30009707.

7: Livingston KE, Mahoney JP, Manglik A, Sunahara RK, Traynor JR. Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. Elife. 2018 Jun 22;7. pii: e32499. doi: 10.7554/eLife.32499. PubMed PMID: 29932421; PubMed Central PMCID: PMC6042960.

8: Hill R, Disney A, Conibear A, Sutcliffe K, Dewey W, Husbands S, Bailey C, Kelly E, Henderson G. The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception. Br J Pharmacol. 2018 Jul;175(13):2653-2661. doi: 10.1111/bph.14224. Epub 2018 May 14. PubMed PMID: 29582414; PubMed Central PMCID: PMC6003631.

9: Badshah SL, Ullah A, Al-Showiman SS, Mabkhot YN. Better agonist for the opioid receptors. Chem Cent J. 2018 Feb 8;12(1):13. doi: 10.1186/s13065-018-0383-8. PubMed PMID: 29417377; PubMed Central PMCID: PMC5803155.

10: Sader S, Anant K, Wu C. To probe interaction of morphine and IBNtxA with 7TM and 6TM variants of the human μ-opioid receptor using all-atom molecular dynamics simulations with an explicit membrane. Phys Chem Chem Phys. 2018 Jan 17;20(3):1724-1741. doi: 10.1039/c7cp06745c. PubMed PMID: 29265141.

11: Cheng JX, Cheng T, Li WH, Liu GX, Zhu WL, Tang Y. Computational insights into the G-protein-biased activation and inactivation mechanisms of the μ opioid receptor. Acta Pharmacol Sin. 2018 Jan;39(1):154-164. doi: 10.1038/aps.2017.158. Epub 2017 Nov 30. PubMed PMID: 29188799; PubMed Central PMCID: PMC5758664.

12: Link A, Müller CE. G-Protein-Coupled Receptors: Sustained Signaling via Intracellular Megaplexes and Pathway-Specific Drugs. Angew Chem Int Ed Engl. 2016 Dec 23;55(52):15962-15964. doi: 10.1002/anie.201609015. Epub 2016 Oct 24. PubMed PMID: 27775210.

13: Kostic M. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology. Cell Chem Biol. 2016 Sep 22;23(9):1039-1040. doi: 10.1016/j.chembiol.2016.09.007. PubMed PMID: 27662248.

14: Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. Epub 2016 Aug 17. PubMed PMID: 27533032; PubMed Central PMCID: PMC5161585.