Tabimorelin

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

MedKoo CAT#: 530201

CAS#: 193079-69-5

Description: Tabimorelin is a growth hormone releasing factor agonist potentially for the treatment of growth hormone deficit. Tabimorelin is a drug which acts as a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue, mimicking the effects of the endogenous peptide agonist ghrelin as a stimulator of growth hormone (GH) release.

Chemical Structure

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Tabimorelin
CAS# 193079-69-5
Instruction

Theoretical Analysis

MedKoo Cat#: 530201
Name: Tabimorelin
CAS#: 193079-69-5
Chemical Formula: C32H40N4O3
Exact Mass: 528.31
Molecular Weight: 528.697
Elemental Analysis: C, 72.70; H, 7.63; N, 10.60; O, 9.08

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.

Request quote for custom synthesis

Synonym: Tabimorelin, NN-703, NNC-26-0703, NNC-260703, NN703, NNC26-0703, NNC260703

IUPAC/Chemical Name: (E)-5-amino-N,5-dimethyl-N-((R)-1-(methyl((R)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)hex-2-enamide

InChi Key: WURGZWOTGMLDJP-ZCYANPAGSA-N

InChi Code: InChI=1S/C32H40N4O3/c1-32(2,33)19-11-16-29(37)35(4)28(22-24-17-18-25-14-9-10-15-26(25)20-24)31(39)36(5)27(30(38)34-3)21-23-12-7-6-8-13-23/h6-18,20,27-28H,19,21-22,33H2,1-5H3,(H,34,38)/b16-11+/t27-,28-/m1/s1

SMILES Code: CC(C)(N)C/C=C/C(N(C)[C@@H](C(N(C)[C@@H](C(NC)=O)CC1=CC=CC=C1)=O)CC2=CC=C3C=CC=CC3=C2)=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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 528.70 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:
In vitro protocol:
In vivo protocol:

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1: Lange T, Thomas A, Görgens C, Bidlingmaier M, Schilbach K, Fichant E, Delahaut P, Thevis M. Comprehensive insights into the formation of metabolites of the ghrelin mimetics capromorelin, macimorelin and tabimorelin as potential markers for doping control purposes. Biomed Chromatogr. 2021 Jun;35(6):e5075. doi: 10.1002/bmc.5075. Epub 2021 Feb 2. PMID: 33458843.


2: Holm AM, Johansen PB, Ahnfelt-Rønne I, Rømer J. Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin- signalling-deficient ZDF rats. Eur J Endocrinol. 2004 Jun;150(6):893-904. doi: 10.1530/eje.0.1500893. PMID: 15191361.


3: Zdravkovic M, Olsen AK, Christiansen T, Schulz R, Taub ME, Thomsen MS, Rasmussen MH, Ilondo MM. A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate. Eur J Clin Pharmacol. 2003 Feb;58(10):683-8. doi: 10.1007/s00228-002-0539-1. Epub 2003 Feb 6. PMID: 12610745.


4: Shimatsu A. [Ghrelin-related drugs: clinical perspectives]. Nihon Rinsho. 2004 Sep;62 Suppl 9:435-8. Japanese. PMID: 15506422.


5: Zdravkovic M, Søgaard B, Ynddal L, Christiansen T, Agersø H, Thomsen MS, Falch JE, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers. Growth Horm IGF Res. 2000 Aug;10(4):193-8. doi: 10.1054/ghir.2000.0152. PMID: 11032702.


6: Zdravkovic M, Christiansen T, Eliot L, Agersoe H, Thomsen MS, Falch JF, Søgaard B, Ynddal L, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects. Growth Horm IGF Res. 2001 Feb;11(1):41-8. doi: 10.1054/ghir.2000.0188. PMID: 11437473.


7: Ahnfelt-Rønne I, Nowak J, Olsen UB. Do growth hormone-releasing peptides act as ghrelin secretagogues? Endocrine. 2001 Feb;14(1):133-5. doi: 10.1385/ENDO:14:1:133. PMID: 11322495.


8: Peschke B, Hansen BS. New growth hormone secretagogues: C-terminal modified sulfonamide-analogues of NN703. Bioorg Med Chem Lett. 1999 May 3;9(9):1295-8. doi: 10.1016/s0960-894x(99)00167-5. PMID: 10340617.


9: Hansen TK, Ankersen M, Raun K, Hansen BS. Highly potent growth hormone secretagogues: hybrids of NN703 and ipamorelin. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1915-8. doi: 10.1016/s0960-894x(01)00345-6. PMID: 11459660.


10: Peschke B, Ankersen M, Bauer M, Hansen TK, Hansen BS, Nielsen KK, Raun K, Richter L, Westergaard L. The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency. Eur J Med Chem. 2002 Jun;37(6):487-501. doi: 10.1016/s0223-5234(02)01370-3. PMID: 12204475.


11: Hansen BS, Raun K, Nielsen KK, Johansen PB, Hansen TK, Peschke B, Lau J, Andersen PH, Ankersen M. Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol. 1999 Aug;141(2):180-9. doi: 10.1530/eje.0.1410180. PMID: 10427162.


12: Svensson J, Monson JP, Vetter T, Hansen TK, Savine R, Kann P, Bex M, Reincke M, Hagen C, Beckers A, Ilondo MM, Zdravkovic M, Bengtsson BA, Korbonits M; NN703 Clinical Research Group. Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency. Clin Endocrinol (Oxf). 2003 May;58(5):572-80. doi: 10.1046/j.1365-2265.2003.01754.x. PMID: 12699438.


13: Ankersen M, Kramer Nielsen K, Kruse Hansen T, Raun K, Sehested Hansen B. Growth hormone secretagogues derived from NN703 with hydrazidesas c-terminal. Eur J Med Chem. 2000 May;35(5):487-97. doi: 10.1016/s0223-5234(00)00146-x. PMID: 10889328.


14: Agersø H, Ynddal L, Søgaard B, Zdravkovic M. Pharmacokinetic and pharmacodynamic modeling of NN703, a growth hormone secretagogue, after a single po dose to human volunteers. J Clin Pharmacol. 2001 Feb;41(2):163-9. doi: 10.1177/00912700122009971. PMID: 11210396.


15: Peschke B, Ankersen M, Hansen TK, Hansen BS, Lau J, Nielsen KK, Raun K. New highly potent dipeptidic growth hormone secretagogues with low molecular weight. Eur J Med Chem. 2000 Jun;35(6):599-618. doi: 10.1016/s0223-5234(00)00160-4. PMID: 10906412.


16: Malmlöf K, Bauer MK, Johansen PB, Ankersen M, Veldhuis JD. Daily low-dose administration of growth hormone secretagogue stimulates pulsatile growth hormone secretion and elevates plasma insulin-like growth factor-1 levels in pigs. Endocrine. 2001 Dec;16(3):195-9. doi: 10.1385/ENDO:16:3:195. PMID: 11954663.


17: Nielsen KK, Buddington KK, Raun K, Hansen TK, Buddington RK. Absorption and systemic availability of two synthetic growth hormone secretogogues and transport of glucose by the proximal small intestine of anestrus dogs after administering estradiol. J Comp Physiol B. 2003 Feb;173(1):61-7. doi: 10.1007/s00360-002-0312-x. Epub 2003 Jan 9. PMID: 12592444.


18: Zdravkovic M, Christiansen T, Grosch K, Ilondo MM. Evaluation of the conformity of human growth hormone concentrations measured with the DPC Immulite and the Nichols Advantage assays. Clin Chem Lab Med. 2000 Aug;38(8):799-800. doi: 10.1515/CCLM.2000.114. PMID: 11071076.