VTP-27999

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MedKoo CAT#: 125293

CAS#: 942142-51-0 (free base)

Description: VTP-27999 is a highly potent and selective renin inhibitor (IC50 = 0.47 nM). VTP-27999 demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans.

Chemical Structure

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VTP-27999
CAS# 942142-51-0 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 125293
Name: VTP-27999
CAS#: 942142-51-0 (free base)
Chemical Formula: C26H41ClN4O5
Exact Mass: 524.28
Molecular Weight: 525.090
Elemental Analysis: C, 59.47; H, 7.87; Cl, 6.75; N, 10.67; O, 15.23

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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Related CAS #: 1013937-63-7 (TFA)   942142-51-0 (free base)   1264191-73-2 (HCl)  

Synonym: VTP-27999; VTP27999; VTP 27999;

IUPAC/Chemical Name: methyl (2-((R)-(3-chlorophenyl)((R)-1-(((S)-2-(methylamino)-3-((R)-tetrahydro-2H-pyran-3-yl)propyl)carbamoyl)piperidin-3-yl)methoxy)ethyl)carbamate

InChi Key: NXWASIVXQMMPLM-ZXMXYHOLSA-N

InChi Code: InChI=1S/C26H41ClN4O5/c1-28-23(14-19-6-5-12-35-18-19)16-30-25(32)31-11-4-8-21(17-31)24(20-7-3-9-22(27)15-20)36-13-10-29-26(33)34-2/h3,7,9,15,19,21,23-24,28H,4-6,8,10-14,16-18H2,1-2H3,(H,29,33)(H,30,32)/t19-,21-,23+,24+/m1/s1

SMILES Code: [H][C@]1(CCCN(C1)C(=O)NC[C@H](C[C@H]2CCCOC2)NC)[C@@H](OCCNC(=O)OC)C3=CC=CC(Cl)=C3

Appearance: To be determined

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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 525.09 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: Barkoudah E, van Thiel BS, Fisher ND, Gregg RA, Danser AH, Moukarbel GV, Hollenberg NK. Maximum renal responses to renin inhibition in healthy study participants: VTP-27999 versus aliskiren. J Hypertens. 2016 May;34(5):935-41. doi: 10.1097/HJH.0000000000000860. PubMed PMID: 26882043.

2: Lu X, Krop M, Batenburg WW, Musterd-Bhaggoe UM, Garrelds IM, Danser AH. Renin inhibitor VTP-27999 differs from aliskiren: focus on their intracellular accumulation and the (pro)renin receptor. J Hypertens. 2014 Jun;32(6):1255-63. doi: 10.1097/HJH.0000000000000167. PubMed PMID: 24637873.

3: Balcarek J, Sevá Pessôa B, Bryson C, Azizi M, Ménard J, Garrelds IM, McGeehan G, Reeves RA, Griffith SG, Danser AH, Gregg R. Multiple ascending dose study with the new renin inhibitor VTP-27999: nephrocentric consequences of too much renin inhibition. Hypertension. 2014 May;63(5):942-50. doi: 10.1161/HYPERTENSIONAHA.113.02893. Epub 2014 Jan 27. PubMed PMID: 24470465.

4: Krop M, Lu X, Verdonk K, Schalekamp MA, van Gool JM, McKeever BM, Gregg R, Danser AH. New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin. Hypertension. 2013 May;61(5):1075-82. doi: 10.1161/HYPERTENSIONAHA.111.00967. Epub 2013 Mar 4. PubMed PMID: 23460288.

5: Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Med Chem
Lett. 2011 Aug 9;2(10):747-51. doi: 10.1021/ml200137x. eCollection 2011 Oct 13.
PubMed PMID: 24900262; PubMed Central PMCID: PMC4018089.