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Relaxin H2 (human)

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Relaxin H2 (human), a recombinant human relaxin targeting the RLN receptor, is a vasoactive peptide hormone with antifibrotic activity. Relaxin H2 is a pregnancy hormone with cardioprotective activity. It is the main storage and circulation subtype of relaxin peptide hormone in humans.

Category

Peptide Inhibitors

Catalog number

BAT-014502

CAS number

99489-94-8

Molecular Formula

C256H408N74O74S8

Molecular Weight

5963.04

Specification
Reference Reading

IUPAC Name

(1R,6R,12S,15S,18S,21S,24S,27S,30S,33S,36S,39S,42R,47R,50S,53S,56S,59S,62S,65S,68S,71S,74R,80S,83S,88R)-6-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-88-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-hydroxy-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-4-methyl-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-68-(4-aminobutyl)-30-(3-amino-3-oxopropyl)-50-benzyl-33,39-bis[(2S)-butan-2-yl]-12,24,53,65-tetrakis(3-carbamimidamidopropyl)-15-(2-carboxyethyl)-42-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-2-oxoethyl]carbamoyl]-71-[(1R)-1-hydroxyethyl]-62-(hydroxymethyl)-83-(1H-imidazol-5-ylmethyl)-27,36,56-trimethyl-18,59-bis(2-methylpropyl)-7,10,13,16,19,22,25,28,31,34,37,40,49,52,55,58,61,64,67,70,73,76,79,82,85,87-hexacosaoxo-21,80-di(propan-2-yl)-3,4,44,45,90,91-hexathia-8,11,14,17,20,23,26,29,32,35,38,41,48,51,54,57,60,63,66,69,72,75,78,81,84,86-hexacosazabicyclo[72.11.7]dononacontane-47-carboxylic acid

Synonyms

Serelaxin; (Pyr-Leu-Tyr-Ser-Ala-Leu-Ala-Asn-Lys-Cys-Cys-His-Val-Gly-Cys-Thr-Lys-Arg-Ser-Leu-Ala-Arg-Phe-Cys-OH)A (H-Asp-Ser-Trp-Met-Glu-Glu-Val-Ile-Lys-Leu-Cys-Gly-Arg-Glu-Leu-Val-Arg-Ala-Gln-Ile-Ala-Ile-Cys-Gly-Met-Ser-Thr-Trp-Ser-OH)B (Disulfide bridge: Cys10A-Cys15A, Cys11A-Cys11B, Cys24A-Cys23B); L-alpha-aspartyl-L-seryl-L-tryptophyl-L-methionyl-L-alpha-glutamyl-L-alpha-glutamyl-L-valyl-L-isoleucyl-L-lysyl-L-leucyl-L-cysteinyl-glycyl-L-arginyl-L-alpha-glutamyl-L-leucyl-L-valyl-L-arginyl-L-alanyl-L-glutaminyl-L-isoleucyl-L-alanyl-L-isoleucyl-L-cysteinyl-glycyl-L-methionyl-L-seryl-L-threonyl-L-tryptophyl-L-serine (11->11'),(23->24')-bis(disulfide) compound with L-pyroglutamyl-L-leucyl-L-tyrosyl-L-seryl-L-alanyl-L-leucyl-L-alanyl-L-asparagyl-L-lysyl-L-cysteinyl-L-cysteinyl-L-histidyl-L-valyl-glycyl-L-cysteinyl-L-threonyl-L-lysyl-L-arginyl-L-seryl-L-leucyl-L-alanyl-L-arginyl-L-phenylalanyl-L-cysteine (10'->15')-disulfide; Human relaxin II

Appearance

White Lyophilized Powder

Purity

≥95% by HPLC

Sequence

(Pyr-LYSALANKCCHVGCTKRSLARFC)A (DSWMEEVIKLCGRELVRAQIAICGMSTWS)B (Disulfide bridge: Cys10A-Cys15A, Cys11A-Cys11B, Cys24A-Cys23B)

Storage

Store at -20°C

Solubility

Soluble in Water

InChI

InChI=1S/C256H408N74O74S8/c1-32-128(20)198-246(396)286-135(27)207(357)326-199(129(21)33-2)248(398)321-180(210(360)279-106-189(343)289-161(79-88-405-30)221(371)315-177(111-334)239(389)329-202(137(29)337)250(400)312-171(232(382)317-178(112-335)251(401)402)98-141-103-277-148-57-41-39-55-145(141)148)114-408-412-118-184(252(403)404)322-230(380)168(95-138-52-36-35-37-53-138)308-215(365)154(63-50-86-274-255(267)268)291-203(353)132(24)283-226(376)164(91-121(6)7)307-238(388)176(110-333)314-216(366)155(64-51-87-275-256(269)270)293-213(363)151(59-43-46-82-258)301-249(399)201(136(28)336)330-242(392)181-115-409-411-117-183(319-217(367)150(58-42-45-81-257)294-233(383)173(101-186(262)340)303-206(356)133(25)284-225(375)163(90-120(4)5)302-205(355)134(26)285-236(386)174(108-331)316-229(379)169(96-139-65-67-143(338)68-66-139)309-227(377)165(92-122(8)9)305-218(368)156-70-75-187(341)287-156)241(391)320-182(240(390)311-172(99-142-104-271-119-281-142)235(385)323-195(125(14)15)243(393)280-107-190(344)290-181)116-410-407-113-179(209(359)278-105-188(342)288-149(61-48-84-272-253(263)264)212(362)295-159(72-77-192(347)348)220(370)306-167(94-124(12)13)234(384)325-196(126(16)17)244(394)299-153(62-49-85-273-254(265)266)211(361)282-131(23)204(354)292-157(224(374)327-198)69-74-185(261)339)318-228(378)166(93-123(10)11)304-214(364)152(60-44-47-83-259)300-247(397)200(130(22)34-3)328-245(395)197(127(18)19)324-223(373)160(73-78-193(349)350)297-219(369)158(71-76-191(345)346)296-222(372)162(80-89-406-31)298-231(381)170(97-140-102-276-147-56-40-38-54-144(140)147)310-237(387)175(109-332)313-208(358)146(260)100-194(351)352/h35-41,52-57,65-68,102-104,119-137,146,149-184,195-202,276-277,331-338H,32-34,42-51,58-64,69-101,105-118,257-260H2,1-31H3,(H2,261,339)(H2,262,340)(H,271,281)(H,278,359)(H,279,360)(H,280,393)(H,282,361)(H,283,376)(H,284,375)(H,285,386)(H,286,396)(H,287,341)(H,288,342)(H,289,343)(H,290,344)(H,291,353)(H,292,354)(H,293,363)(H,294,383)(H,295,362)(H,296,372)(H,297,369)(H,298,381)(H,299,394)(H,300,397)(H,301,399)(H,302,355)(H,303,356)(H,304,364)(H,305,368)(H,306,370)(H,307,388)(H,308,365)(H,309,377)(H,310,387)(H,311,390)(H,312,400)(H,313,358)(H,314,366)(H,315,371)(H,316,379)(H,317,382)(H,318,378)(H,319,367)(H,320,391)(H,321,398)(H,322,380)(H,323,385)(H,324,373)(H,325,384)(H,326,357)(H,327,374)(H,328,395)(H,329,389)(H,330,392)(H,345,346)(H,347,348)(H,349,350)(H,351,352)(H,401,402)(H,403,404)(H4,263,264,272)(H4,265,266,273)(H4,267,268,274)(H4,269,270,275)/t128-,129-,130-,131-,132-,133-,134-,135-,136+,137+,146-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-,168-,169-,170-,171-,172-,173-,174-,175-,176-,177-,178-,179-,180-,181-,182-,183-,184-,195-,196-,197-,198-,199-,200-,201-,202-/m0/s1

InChI Key

DTLOVISJEFBXLX-REAFJZEQSA-N

Canonical SMILES

CCC(C)C1C(=O)NC(CSSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C2CSSCC(C(=O)NC(CSSCC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)C)C(C)CC)CCC(=O)N)C)CCCNC(=N)N)C(C)C)CC(C)C)CCC(=O)O)CCCNC(=N)N)NC(=O)C(CC(C)C)NC(=O)C(CCCCN)NC(=O)C(C(C)CC)NC(=O)C(C(C)C)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CO)NC(=O)C(CC(=O)O)N)C(=O)NC(C(=O)NC(C(=O)NCC(=O)N2)C(C)C)CC5=CN=CN5)NC(=O)C(CCCCN)NC(=O)C(CC(=O)N)NC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CO)NC(=O)C(CC6=CC=C(C=C6)O)NC(=O)C(CC(C)C)NC(=O)C7CCC(=O)N7)C(C)O)CCCCN)CCCNC(=N)N)CO)CC(C)C)C)CCCNC(=N)N)CC8=CC=CC=C8)C(=O)O)C(=O)NCC(=O)NC(CCSC)C(=O)NC(CO)C(=O)NC(C(C)O)C(=O)NC(CC9=CNC1=CC=CC=C19)C(=O)NC(CO)C(=O)O

1. Recombinant human H2 relaxin (serelaxin) as a cardiovascular drug: aiming at the right target

Daniele Bani Drug Discov Today. 2020 Jul;25(7):1239-1244. doi: 10.1016/j.drudis.2020.04.014. Epub 2020 Apr 29.

Serelaxin (recombinant human relaxin-2 hormone; RLX-2) had raised expectations as a new medication for cardiovascular diseases. Evidence from preclinical studies indicated that serelaxin has chronotropic, inotropic, and anti-arrhythmic actions on the myocardium and cardioprotective effects mediated by vasodilation, angiogenesis, and inhibition of inflammation and fibrosis. However, clinical trials with serelaxin in patients with acute heart failure (AHF) gave inconclusive results. A critical reappraisal of the comprehensive cardiovascular actions of serelaxin clearly delineates acute myocardial infarction (AMI) as a feasible therapeutic target. Serelaxin acts at multiple levels on the pathogenic mechanisms of AMI and previous in vivo studies suggest that its administration at reperfusion affords myocardial salvage. Thus, serelaxin could be an effective adjunctive medical therapy to coronary angioplasty.

2. Commercial immunoassays for human relaxin-2

Dennis R Stewart Mol Cell Endocrinol. 2019 May 1;487:94-97. doi: 10.1016/j.mce.2019.01.004. Epub 2019 Jan 8.

Several different immunoassays have been used in the commercial pharmaceutical development of serelaxin. These assays have been well validated for submission of GLP preclinical and clinical studies to the FDA and EU regulatory bodies. The requirements for these assays exceed that of most research assays commonly developed in academic research but have been and are currently available to academic researchers. Additionally, many human relaxin immunoassays are commercially available from a variety of vendors. Validation procedures for immunoassays are well understood and documented, however validation of these assays is often lacking or completely absent. The data derived from these assays must be questioned if the investigator does not supply information on the validation of the assay used, either from the supplier or through their own efforts. Many recent papers on determination of serum relaxin in clinical settings have recently been published. The assay used for this determination varies but generally is one of two commercially available. These manuscripts and the assay used is discussed. Direct comparisons of assays are lacking but some general conclusions can be drawn by comparing results from similar studies using different assays. There is disagreement among the results of the concentrations of serum relaxin from the use of different assays that raise questions on assay reliability. The differences in the quality of immunoassays used for detection of serum relaxin should be part of the decisions making process in choosing an assay. While the end user bears the ultimate responsibility to demonstrate the assay is valid for the stated claims, reviewers and editors also share responsibility for quality of published results.

3. Production of human pro-relaxin H2 in the yeast Pichia pastoris

D Cimini, et al. BMC Biotechnol. 2017 Jan 14;17(1):4. doi: 10.1186/s12896-016-0319-0.

Background: Initially known as the reproductive hormone, relaxin was shown to possess other therapeutically useful properties that include extracellular matrix remodeling, anti-inflammatory, anti-ischemic and angiogenic effects. All these findings make relaxin a potential drug for diverse medical applications. Its precursor, pro-relaxin, is an 18 kDa protein, that shows activity in in vitro assays. Since extraction of relaxin from animal tissues raises several issues, prokaryotes and eukaryotes were both used as expression systems for recombinant relaxin production. Most productive results were obtained when using Escherichia coli as a host for human relaxin expression. However, in such host, relaxin precipitated in the form of inclusion bodies and, therefore, required several expensive recovery steps as cell lysis, refolding and reduction. Results: To overcome the issues related to prokaryotic expression here we report the production and purification of secreted human pro-relaxin H2 by using the methylotrophic yeast Pichia pastoris as expression host. The methanol inducible promoter AOX1 was used to drive expression of the native and histidine tagged forms of pro-relaxin H2 in dual phase fed-batch experiments on the 22 L scale. Both protein forms presented the correct structure, as determined by mass spectrometry and western blotting analyses, and demonstrated to be biologically active in immune enzymatic assays. The presence of the tag allowed to simplify pro-relaxin purification obtaining higher purity. Conclusions: This work presents a strategy for microbial production of recombinant human pro-relaxin H2 in Pichia pastoris that allowed the obtainment of biologically active pro-hormone, with a final concentration in the fermentation broth ranging between 10 and 14 mg/L of product, as determined by densitometric analyses.